Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
Inhibitors of reverse transcriptase (RNA-DIRECTED DNA POLYMERASE), an enzyme that synthesizes DNA on an RNA template.
A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.
The type species of LENTIVIRUS and the etiologic agent of AIDS. It is characterized by its cytopathic effect and affinity for the T4-lymphocyte.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
An antibiotic purine ribonucleoside that readily substitutes for adenosine in the biological system, but its incorporation into DNA and RNA has an inhibitory effect on the metabolism of these nucleic acids.
The ability of viruses to resist or to become tolerant to chemotherapeutic agents or antiviral agents. This resistance is acquired through gene mutation.
A disorder present in the newborn infant in which constriction rings or bands, causing soft tissue depressions, encircle digits, extremities, or limbs and sometimes the neck, thorax, or abdomen. They may be associated with intrauterine amputations.
OXAZINES with a fused BENZENE ring.
Congenital malformations of the central nervous system and adjacent structures related to defective neural tube closure during the first trimester of pregnancy generally occurring between days 18-29 of gestation. Ectodermal and mesodermal malformations (mainly involving the skull and vertebrae) may occur as a result of defects of neural tube closure. (From Joynt, Clinical Neurology, 1992, Ch55, pp31-41)
Congenital abnormalities caused by medicinal substances or drugs of abuse given to or taken by the mother, or to which she is inadvertently exposed during the manufacture of such substances. The concept excludes abnormalities resulting from exposure to non-medicinal chemicals in the environment.
An umbrella term used to describe a pattern of disabilities and abnormalities that result from fetal exposure to ETHANOL during pregnancy. It encompasses a phenotypic range that can vary greatly between individuals, but reliably includes one or more of the following: characteristic facial dysmorphism, FETAL GROWTH RETARDATION, central nervous system abnormalities, cognitive and/or behavioral dysfunction, BIRTH DEFECTS. The level of maternal alcohol consumption does not necessarily correlate directly with disease severity.
Severe or complete loss of facial muscle motor function. This condition may result from central or peripheral lesions. Damage to CNS motor pathways from the cerebral cortex to the facial nuclei in the pons leads to facial weakness that generally spares the forehead muscles. FACIAL NERVE DISEASES generally results in generalized hemifacial weakness. NEUROMUSCULAR JUNCTION DISEASES and MUSCULAR DISEASES may also cause facial paralysis or paresis.
The beginning third of a human PREGNANCY, from the first day of the last normal menstrual period (MENSTRUATION) through the completion of 14 weeks (98 days) of gestation.
A reverse transcriptase encoded by the POL GENE of HIV. It is a heterodimer of 66 kDa and 51 kDa subunits that are derived from a common precursor protein. The heterodimer also includes an RNAse H activity (RIBONUCLEASE H, HUMAN IMMUNODEFICIENCY VIRUS) that plays an essential role the viral replication process.
The former British crown colony located off the southeast coast of China, comprised of Hong Kong Island, Kowloon Peninsula, and New Territories. The three sites were ceded to the British by the Chinese respectively in 1841, 1860, and 1898. Hong Kong reverted to China in July 1997. The name represents the Cantonese pronunciation of the Chinese xianggang, fragrant port, from xiang, perfume and gang, port or harbor, with reference to its currents sweetened by fresh water from a river west of it.
Agents used to treat AIDS and/or stop the spread of the HIV infection. These do not include drugs used to treat symptoms or opportunistic infections associated with AIDS.
A quantitative prediction of the biological, ecotoxicological or pharmaceutical activity of a molecule. It is based upon structure and activity information gathered from a series of similar compounds.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture.
Lists of words, usually in alphabetical order, giving information about form, pronunciation, etymology, grammar, and meaning.
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).
Purine or pyrimidine bases attached to a ribose or deoxyribose. (From King & Stansfield, A Dictionary of Genetics, 4th ed)
Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.
Virus infection of the Gasserian ganglion and its nerve branches characterized by pain and vesicular eruptions with much swelling. Ocular involvement is usually heralded by a vesicle on the tip of the nose. This area is innervated by the nasociliary nerve.
A common, benign, usually self-limited viral infection of the skin and occasionally the conjunctivae by a poxvirus (MOLLUSCUM CONTAGIOSUM VIRUS). (Dorland, 27th ed)
A species of MOLLUSCIPOXVIRUS causing skin lesions in humans. It is transmitted by direct contact or from non-living reservoirs (fomites), such as books or clothing.
A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.
An acute infectious, usually self-limited, disease believed to represent activation of latent varicella-zoster virus (HERPESVIRUS 3, HUMAN) in those who have been rendered partially immune after a previous attack of CHICKENPOX. It involves the SENSORY GANGLIA and their areas of innervation and is characterized by severe neuralgic pain along the distribution of the affected nerve and crops of clustered vesicles over the area. (From Dorland, 27th ed)
Paralysis of one or more of the ocular muscles due to disorders of the eye muscles, neuromuscular junction, supporting soft tissue, tendons, or innervation to the muscles.
A body of water covering approximately one-fifth of the total ocean area of the earth, extending amidst Africa in the west, Australia in the east, Asia in the north, and Antarctica in the south. Including the Red Sea and the Persian Gulf, it constitutes the third largest ocean after the ATLANTIC OCEAN and the PACIFIC OCEAN. (New Encyclopaedia Britannica Micropaedia, 15th ed, 1990, p289)
A publication issued at stated, more or less regular, intervals.
A bibliographic database that includes MEDLINE as its primary subset. It is produced by the National Center for Biotechnology Information (NCBI), part of the NATIONAL LIBRARY OF MEDICINE. PubMed, which is searchable through NLM's Web site, also includes access to additional citations to selected life sciences journals not in MEDLINE, and links to other resources such as the full-text of articles at participating publishers' Web sites, NCBI's molecular biology databases, and PubMed Central.
"The business or profession of the commercial production and issuance of literature" (Webster's 3d). It includes the publisher, publication processes, editing and editors. Production may be by conventional printing methods or by electronic publishing.
Enzymes that catalyze DNA template-directed extension of the 3'-end of an RNA strand one nucleotide at a time. They can initiate a chain de novo. In eukaryotes, three forms of the enzyme have been distinguished on the basis of sensitivity to alpha-amanitin, and the type of RNA synthesized. (From Enzyme Nomenclature, 1992).
Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses).
Substances that reduce the growth or reproduction of BACTERIA.
Substances that destroy fungi by suppressing their ability to grow or reproduce. They differ from FUNGICIDES, INDUSTRIAL because they defend against fungi present in human or animal tissues.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
A species of STAPHYLOCOCCUS that is a spherical, non-motile, gram-positive, chemoorganotrophic, facultative anaerobe. Mainly found on the skin and mucous membrane of warm-blooded animals, it can be primary pathogen or secondary invader.

Inhibition of human immunodeficiency virus type 1 replication by combination of transcription inhibitor K-12 and other antiretroviral agents in acutely and chronically infected cells. (1/2177)

8-Difluoromethoxy-1-ethyl-6-fluoro-1,4-dihydro-7-[4-(2-methoxyp hen yl)-1- piperazinyl]-4-oxoquinoline-3-carboxylic acid (K-12) has recently been identified as a potent and selective inhibitor of human immunodeficiency virus type 1 (HIV-1) transcription. In this study, we examined several combinations of K-12 and other antiretroviral agents for their inhibitory effects on HIV-1 replication in acutely and chronically infected cell cultures. Combinations of K-12 and a reverse transcriptase (RT) inhibitor, either zidovudine, lamivudine, or nevirapine, synergistically inhibited HIV-1 replication in acutely infected MT-4 cells. The combination of K-12 and the protease inhibitor nelfinavir (NFV) also synergistically inhibited HIV-1, whereas the synergism of this combination was weaker than that of the combinations with the RT inhibitors. K-12 did not enhance the cytotoxicities of RT and protease inhibitors. Synergism of the combinations was also observed in acutely infected peripheral blood mononuclear cells. The combination of K-12 and cepharanthine, a nuclear factor kappa B inhibitor, synergistically inhibited HIV-1 production in tumor necrosis factor alpha-stimulated U1 cells, a promonocytic cell line chronically infected with the virus. In contrast, additive inhibition was observed for the combination of K-12 and NFV. These results indicate that the combinations of K-12 and clinically available antiretroviral agents may have potential as chemotherapeutic modalities for the treatment of HIV-1 infection.  (+info)

Safety and pharmacokinetics of abacavir (1592U89) following oral administration of escalating single doses in human immunodeficiency virus type 1-infected adults. (2/2177)

Abacavir (1592U89) is a nucleoside analog reverse transcriptase inhibitor that has been demonstrated to have selective activity against human immunodeficiency virus (HIV) in vitro and favorable safety profiles in mice and monkeys. A phase I study was conducted to evaluate the safety and pharmacokinetics of abacavir following oral administration of single escalating doses (100, 300, 600, 900, and 1,200 mg) to HIV-infected adults. In this double-blind, placebo-controlled study, subjects with baseline CD4+ cell counts ranging from < 50 to 713 cells per mm3 (median, 315 cells per mm3) were randomly assigned to receive abacavir (n = 12) or placebo (n = 6). The bioavailability of the caplet formulation relative to that of the oral solution was also assessed with the 300-mg dose. Abacavir was well tolerated by all subjects; mild to moderate asthenia, abdominal pain, headache, diarrhea, and dyspepsia were the most frequently reported adverse events, and these were not dose related. No significant clinical or laboratory abnormalities were observed throughout the study. All doses resulted in mean abacavir concentrations in plasma that exceeded the mean 50% inhibitory concentration (IC50) for clinical HIV isolates in vitro (0.07 microgram/ml) for almost 3 h. Abacavir was rapidly absorbed following oral administration, with the time to the peak concentration in plasma occurring at 1.0 to 1.7 h postdosing. Mean maximum concentrations in plasma (Cmax) and the area under the plasma concentration-time curve from time zero to infinity (AUC0-infinity) increased slightly more than proportionally from 100 to 600 mg (from 0.6 to 4.7 micrograms/ml for Cmax; from 1.0 to 15.7 micrograms.h/ml for AUC0-infinity) but increased proportionally from 600 to 1,200 mg (from 4.7 to 9.6 micrograms/ml for Cmax; from 15.7 to 32.8 micrograms.h/ml for AUC0-infinity. The elimination of abacavir from plasma was rapid, with an apparent elimination half-life of 0.9 to 1.7 h. Abacavir was well absorbed, with a relative bioavailability of the caplet formulation of 96% versus that of an oral solution (drug substance in water). In conclusion, this study showed that abacavir is safe and is well tolerated by HIV-infected subjects and demonstrated predictable pharmacokinetic characteristics when it was administered as single oral doses ranging from 100 to 1,200 mg.  (+info)

Safety and single-dose pharmacokinetics of abacavir (1592U89) in human immunodeficiency virus type 1-infected children. (3/2177)

Abacavir (formerly 1592U89) is a potent 2'-deoxyguanosine analog reverse transcriptase inhibitor that has been demonstrated to have a favorable safety profile in initial clinical trials with adults with human immunodeficiency virus (HIV) type 1 infection. A phase I study was conducted to evaluate the pharmacokinetics and safety of abacavir following the administration of two single oral doses (4 and 8 mg/kg of body weight) to 22 HIV-infected children ages 3 months to 13 years. Plasma was collected for analysis at predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, and 8 h after the administration of each dose. Plasma abacavir concentrations were determined by high-performance liquid chromatography, and data were analyzed by noncompartmental methods. Abacavir was well tolerated by all subjects. The single abacavir-related adverse event was rash, which occurred in 2 of 22 subjects. After administration of the oral solution, abacavir was rapidly absorbed, with the time to the peak concentration in plasma occurring within 1.5 h postdosing. Pharmacokinetic parameter estimates were comparable among the different age groups for each dose level. The mean maximum concentration in plasma (Cmax) and the mean area under the curve from time zero to infinity (AUC0-infinity) increased by 16 and 45% more than predicted, respectively, as the abacavir dose was doubled from 4 to 8 mg/kg (Cmax increased from 1.69 to 3.94 micrograms/ml, and AUC0-infinity increased from 2.82 to 8.09 micrograms.h/ml). Abacavir was rapidly eliminated, with a mean elimination half-life of 0.98 to 1.13 h. The mean apparent clearance from plasma decreased from 27.35 to 18.88 ml/min/kg as the dose increased. Neither body surface area nor creatinine clearance were correlated with pharmacokinetic estimates at either dose. The extent of exposure to abacavir appears to be slightly lower in children than in adults, with the comparable unit doses being based on body weight. In conclusion, this study showed that abacavir is safe and well tolerated in children when it is administered as a single oral dose of 4 or 8 mg/kg.  (+info)

Suppression of replication of multidrug-resistant HIV type 1 variants by combinations of thymidylate synthase inhibitors with zidovudine or stavudine. (4/2177)

The replication of recombinant multidrug-resistant HIV-1 clones modeled on clinically derived resistant HIV-1 strains from patients receiving long-term combination therapy with zidovudine (AZT) plus 2',3'-dideoxycytidine was found to regain sensitivity to AZT and stavudine (D4T) as a consequence of a pharmacologically induced decrease in de novo dTMP synthesis. The host-cell system used was phytohemagglutinin-stimulated peripheral blood mononuclear cells; dTMP and dTTP depletion were induced by single exposures to a low level of the thymidylate synthase inhibitor 5-fluorouracil (5-FU) or its deoxynucleoside, 2'-deoxy-5-fluorouridine. The host-cell response to the latter was biphasic: a very rapid decrease in the rate of de novo dTMP formation and, consequently, in intracellular dTTP pools, followed by slower recovery in both indices over 3 to 24 h. With the additional presence of AZT or D4T, however, replication of the multidrug-resistant HIV-1 strains remained inhibited, indicating dependence of HIV DNA chain termination by AZT-5'-monophosphate or 2',3'-didehydro-2', 3'-dideoxythymidine-5'-monophosphate in these resistant strains on simultaneous inhibition of host-cell de novo synthesis of thymidine nucleotides. No effect on viability of control (uninfected) phytohemagglutinin-stimulated/peripheral blood mononuclear cells was noted on 6-day exposures to 5-FU or 2'-deoxy-5-fluorouridine alone or in combination with AZT or D4T, even at drug levels severalfold higher than those used in the viral inhibition studies. These studies may provide useful information for the potential clinical use of AZT/5-FU or D4T/5-FU combinations for the prevention or reversal of multidrug resistance associated with long-term dideoxynucleoside combination therapy.  (+info)

Functional analysis of mutations conferring lamivudine resistance on hepatitis B virus. (5/2177)

Two patterns of mutation are commonly observed in the polymerase gene of lamivudine [(-)2'-deoxy-3'-thiacytidine]-resistant hepatitis B virus (HBV). The M539I substitution in the conserved YMDD motif occurs independently of other changes, whereas the M539V substitution is associated with an additional upstream change (L515M). These mutations were introduced into a common background and their effects on HBV DNA replication and lamivudine resistance studied. The L515M and M539V mutations provided only partial resistance while the M539I mutation conferred a high degree of lamivudine resistance. The combination of the L515M and M539V mutations gave an intermediate level of replication competence, compared with either mutation alone, and increased resistance to lamivudine. This probably accounts for these two mutations always being observed together. The M539I mutation reduced replication competence.  (+info)

The cost-effectiveness of treatment with lamivudine and zidovudine compared with zidovudine alone: a comparison of Markov model and trial data estimates. (6/2177)

In this paper, we present a Markov model for estimating the cost-effectiveness of combination therapy with lamivudine (LMV) and zidovudine (ZDV) compared with ZDV alone. We also compare the predictions of the Markov model for the impact of combination therapy on trial period costs with the actual impact of combination therapy on selected trial period costs estimated from data collected during the clinical trials. In the Markov model, disease stages were defined by CD4 cell count. Based on clinical trial data for patients with CD4 counts higher than 100 cells/mm3, the model assumed that the CD4 cell count level could be maintained above the level at the initiation of therapy for 6.5 months with monotherapy and for 18 months with combination therapy. After this period, transition rates for natural disease progression were used. Incremental lifetime costs and quality-adjusted life years gained with LMV/ZDV compared with ZDV alone were estimated for cohorts of patients initiating antiretroviral therapy at four different CD4 cell count stages. Cost per life year gained varied from $10,000 to $18,000, and cost per quality-adjusted life year gained varied from $14,000 to $27,000. In both cases, the combination therapy was more cost-effective when started earlier in disease progression. These estimates were not sensitive to changes in key parameter values. In addition, the model was used to estimate the impact of combination therapy on healthcare costs during the trial period; these estimated costs were compared with data on the cost of resource use collected during the clinical trial for hospital stays, unscheduled visits, medications, and outpatient procedures. Both the Markov model estimates and the trial data estimates for the trial period showed cost savings in other medical costs, though these were not large enough to completely offset the increased cost for antiretroviral therapy. The model estimates were more conservative than the estimates based on the trial data.  (+info)

Antiviral effect and pharmacokinetic interaction between nevirapine and indinavir in persons infected with human immunodeficiency virus type 1. (7/2177)

Nevirapine and indinavir have the potential of affecting the pharmacokinetics of each other. In a prospective trial, 24 human immunodeficiency virus (HIV)-infected subjects on stable nucleoside or no therapy were treated with 800 mg of indinavir every 8 h. After 7 days, 200 mg of nevirapine a day was added for 14 days and then increased to 200 mg twice a day. At day 7 (before nevirapine), there was a sevenfold difference among the subjects in indinavir area under the curve (AUC), and there was a significant correlation between indinavir AUC (r2=0.378, P=.019), minimum plasma concentration (Cmin; r2=0.359, P=.023), maximum plasma concentration (Cmax; r2=0.340, P=.028), and plasma HIV RNA decline. Nevirapine significantly reduced median indinavir Cmin (47.5%) and AUC (27.4%) and, to a lesser extent, Cmax (11%). Plasma HIV RNA values were +info)

Genotypic resistance and the treatment of HIV-1 infection in Espirito Santo, Brazil. (8/2177)

Before December 1997, in Espirito Santo, Brazil, combination antiretroviral therapy was used without routine virologic or immunologic monitoring. To examine consequences of therapy in this setting, clinical information, human immunodeficiency virus type 1 (HIV-1) RNA levels, CD4 cell counts, and protease and reverse transcriptase sequences were determined for consecutive HIV-1-infected outpatients. Of 48 treatment-naive individuals, 11 were started on therapy for HIV-related symptoms; however, 44 (92%) had an RNA level >20,000 copies/mL, a CD4 cell count <500/mm3, or symptoms. Eighteen (51%) of 35 patients on therapy had an RNA level >20,000 copies/mL. Nucleoside-resistance mutations were observed in 21 (68%) of 31 nucleoside-experienced subjects. Protease mutations necessary for high-level protease inhibitor (PI) resistance were present together with permissive mutations in 3 of 10 PI-experienced patients. Inability to identify high-risk individuals and to detect virologic failure may limit the effectiveness of antiretroviral drug programs and may promote the spread of drug resistance where virologic and immunologic monitoring are not available.  (+info)

Information on antiretroviral dosing errors among health care providers for outpatient human immunodeficiency virus (HIV)-infected patients is lacking. We evaluated factors associated with nucleoside reverse-transcriptase inhibitor dosing errors in a university-based HIV clinic using an electronic medical record. Overall, older age, minority race or ethnicity, and didanosine use were related to such errors. Impaired renal function was more common in older patients and racial or ethnic minorities and, in conjunction with fixed-dose combination drugs, contributed to the higher rates of errors in nucleoside reverse-transcriptase inhibitor dosing. Understanding the factors related to nucleoside reverse-transcriptase inhibitor dosing errors is an important step in the building of preventive tools.
Definition of nucleoside reverse transcriptase inhibitor in the Legal Dictionary - by Free online English dictionary and encyclopedia. What is nucleoside reverse transcriptase inhibitor? Meaning of nucleoside reverse transcriptase inhibitor as a legal term. What does nucleoside reverse transcriptase inhibitor mean in law?
Definition of reverse transcriptase inhibitor in the Legal Dictionary - by Free online English dictionary and encyclopedia. What is reverse transcriptase inhibitor? Meaning of reverse transcriptase inhibitor as a legal term. What does reverse transcriptase inhibitor mean in law?
Background: Consistent long-term viral suppression has been difficult to achieve in children with human immunodeficiency virus type 1 (HIV-1) infection. We tested the safety and antiviral efficacy of a novel combination consisting of efavirenz, nelfinavir, and one or more nucleoside reverse-transcriptase inhibitors in 57 children previously treated with only nucleoside reverse-transcriptase inhibitors. Methods: The children were monitored for 48 weeks after the initiation of therapy. We assessed plasma concentrations of efavirenz and nelfinavir, plasma HIV-1 RNA levels, and lymphocyte subpopulations. Results: At base line, the 57 HIV-1â€infected children (age range, 3.8 to 16.8 years) had a median of 699 CD4 cells per cubic millimeter and 10,000 copies of HIV-1 RNA per milliliter of plasma. The most common treatment-related effects of at least moderate severity were rash (in 30 percent of children), diarrhea (in 18 percent), neutropenia (in 12 percent), and biochemical abnormalities (in 12 ...
PubMed Central Canada (PMC Canada) provides free access to a stable and permanent online digital archive of full-text, peer-reviewed health and life sciences research publications. It builds on PubMed Central (PMC), the U.S. National Institutes of Health (NIH) free digital archive of biomedical and life sciences journal literature and is a member of the broader PMC International (PMCI) network of e-repositories.
Tang MW., Rhee S-Y., Bertagnolio S., Ford N., Holmes S., Sigaloff KC., Hamers RL., de Wit TFR., Fleury HJ., Kanki PJ., Ruxrungtham K., Hawkins CA., Wallis CL., Stevens W., van Zyl GU., Manosuthi W., Hosseinipour MC., Ngo-Giang-Huong N., Belec L., Peeters M., Aghokeng A., Bunupuradah T., Burda S., Cane P., Cappelli G., Charpentier C., Dagnra AY., Deshpande AK., El-Katib Z., Eshleman SH., Fokam J., Gody J-C., Katzenstein D., Koyalta DD., Kumwenda JJ., Lallemant M., Lynen L., Marconi VC., Margot NA., Moussa S., Ndungu T., Nyambi PN., Orrell C., Schapiro JM., Schuurman R., Sirivichayakul S., Smith D., Zolfo M., Jordan MR., Shafer RW ...
NRTIs (nucleoside reverse transcriptase inhibitors) are active inhibitors of reverse transcriptase found in retroviruses such as the human immunodeficiency virus (HIV). The different nucleoside reverse transcriptase inhibitors may be activated differently but they have the same mechanism of action. NRTIs are activated generally by phosphorylation to the triphosphate form by cellular enzymes. It then competes with cellular triphosphates, which are substrates for proviral DNA by viral reverse transcriptase. Reverse-transcriptase inhibitors (RTIs) are a class of antiretroviral drugs used to treat HIV infection or AIDS, and in some cases hepatitis B. RTIs inhibit activity of reverse transcriptase, a viral DNA polymerase that is required for replication of HIV and other retroviruses.
BACKGROUND: Understanding the selection and decay of drug-resistant HIV-1 variants is important for designing optimal antiretroviral therapy.. OBJECTIVE: To develop a high-throughput, real-time reverse transcriptase (RT) polymerase chain reaction (PCR) assay to quantify non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant variants K103N (AAT or AAC alleles) at frequencies as low as 0.1%, and to apply this to monitor these variants before, during, and after NNRTI therapy.. METHODS: HIV-1 RNA in longitudinal plasma samples obtained from patients starting and stopping NNRTI therapy was converted to cDNA and the target sequence region amplified and quantified by real-time PCR. Approximately 10 copies/reaction provided a template for a second round of PCR using primers that discriminated between the mutant and wild-type alleles. Amplification specificity was confirmed by thermal denaturation analysis.. RESULTS: Frequencies of 103N similar to assay background (0.029%) were observed in ...
Clinical Pharmacokinetics and Antiviral Activity of CC-31244, a Pan-genotypic, Potent Nonnucleoside NS5B Polymerase Inhibitor (NNI) for the Treatment of Hepatitis C ...
Single dose nevirapine (SD NVP) has greatly reduced the rate of mother-to-child transmission (MTCT) of HIV. Non-nucleoside reverse transcriptase inhibitor (NNRTI)-based regimens are recommended for use by the World Health Organization (WHO) in resource-limited settings. However, research suggests that mothers and infants exposed to SD NVP experience higher virologic failure rates when treated with NNRTI-based regimens than their unexposed counterparts. Data show that the use of SD NVP is associated with NNRTI resistance in HIV infected women and infants. The purpose of this trial was to compare and evaluate virologic responses to an NNRTI-based regimen versus a protease-inhibitor (PI)-based regimen in HIV infected infants who had or had not been exposed to SD NVP intrapartum and after birth.. ,,. ,, Participants were enrolled into one of two Cohorts with proposed enrollment into each Cohort of 288 participants. Cohort I participants must have received SD NVP for prevention of MTCT. Cohort II ...
Gastrointestinal side effects of HAART are usually well tolerated and do not contribute to significant treatment discontinuation. However, diarrhea of moderate to severe intensity can occur in patients receiving multi-drug therapy [21-23]. The mechanisms underlying antiretroviral-induced diarrhea are unclear. The intestinal epithelium acts as a highly selective barrier, preventing the passage of toxic molecules and luminal bacterial translocation [24]. The normal barrier function is maintained by steady enterocyte turnover finely regulated by cell proliferation, migration, and apoptosis. Cell-to-cell contacts within the intestinal epithelium structured by a scaffold of tight and adherens junctions, located apically, are further responsible for sealing the intestinal barrier [25-27]. The results of this study suggest that selected antiretroviral drugs influence small intestinal absorptive and secretory functions.. We have assessed intestinal mucosal morphology, permeability changes, and ...
The study is designed to select a dose of GSK1265744 primarily on the basis of antiviral activity and tolerability in HIV-1 infected, antiretroviral naive subjects.. This study consists of two parts:. Induction Phase: Approximately 200 subjects will be randomized (50 subjects in each of the 4 treatment arms). The Induction Phase consists of a 24 week dose-ranging evaluation of GSK1265744 at blinded doses of 10 mg, 30 mg and 60 mg once-daily and a control arm of open-label efavirenz (EFV) 600 mg once daily. The background dual nucleoside reverse transcriptase inhibitor (NRTI) antiretroviral therapy (ART) for all arms will be either abacavir/lamivudine (ABC/3TC) or tenofovir/emtricitabine (TDF/FTC) as selected by the Investigator. Subjects randomized to a GSK1265744 containing arm, who successfully complete 24 weeks on study and demonstrate virologic suppression (defined as having a plasma HIV-1 ribonucleic acid [RNA] ,50 copies per milliliter [c/mL] before Week 24, with no signs of virologic ...
TY - JOUR. T1 - Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. AU - Famiglini, Valeria. AU - La Regina, Giuseppe. AU - Coluccia, Antonio. AU - Masci, Domiziana. AU - Brancale, Andrea. AU - Badia, Roger. AU - Riveira-Muñoz, Eva. AU - Esté, José A.. AU - Crespan, Emmanuele. AU - Brambilla, Alessandro. AU - Maga, Giovanni. AU - Catalano, Myriam. AU - Limatola, Cristina. AU - Formica, Francesca Romana. AU - Cirilli, Roberto. AU - Novellino, Ettore. AU - Silvestri, Romano. PY - 2017/8/10. Y1 - 2017/8/10. N2 - We designed and synthesized a series of chiral indolyarylsulfones (IASs) as new HIV-1 NNRTIs. The new IASs 8-37 showed potent inhibition of the HIV-1 WT NL4-3 strain and of the mutant K103N, Y181C, Y188L, and K103N-Y181C HIV-1 strains. Six racemic mixtures, 8, 23-25, 31, and 33, were separated at semipreparative level into their pure enantiomers. The (R)-8 enantiomer bearing the chiral (α-methylbenzyl) was ...
Panel of prototypical infectious molecular HIV-1 clones containing multiple nucleoside reverse transcriptase inhibitor resistance mutations ...
Pre-incubation of cell-free HIV-1 group M isolates with non-nucleoside reverse transcriptase inhibitors blocks subsequent viral replication in co-cultures of dendritic cells and T cells ...
We restricted our analyses to patients receiving the common ART combination of nucleoside plus non-nucleoside reverse transcriptase inhibitors. We concentrated on this treatment regimen for two major reasons. Firstly, NRTI plus NNRTI regimens are likely to remain popular as first-line therapy because of their demonstrated efficacy, simplicity of therapy, pill number and tolerability [1]. Secondly, NNRTI/NRTI therapy is likely to remain the dominant regimen for first-line therapy in resource-constrained countries. Among the 42 antiretroviral products whose price the Clinton foundation negotiated for resource-constrained countries only two contain PIs [35]. There are 71 countries (including the vast majority of sub-Saharan countries) that can now benefit from this negotiation, representing more than 92% of the people living with HIV globally [36, 37]. It is important to note that, as a general trend, PIs are likely to remain prohibitively expensive for resource-constrained countries in the short ...
Objective: Receptive anal intercourse in both men and women is associated with the highest probability for sexual acquisition of HIV infection. As part of a program to develop an effective prevention strategy, we performed an ex-vivo preclinical evaluation to determine the efficacy of multiple double combinations of maraviroc (MVC) and reverse transcriptase inhibitors (RTIs). Design: The entry inhibitor, MVC, a nucleotide RTI, tenofovir and two non-nucleoside RTIs, UC781 and TMC120 (dapivirine, DPV), were used in double, combinations against a panel of CCR5-using clade B and clade C HIV-1 isolates and against MVC-escape variants. A gel-formulated version of MVC-DPV combination was also tested. Methods: Indicator cells, cocultures of immature dendritic cells with CD4+T cells, and colorectal tissue explants were used to assess antiviral activity of drug combinations. Results: All dual MVC-RTI combinations tested inhibited MVC-sensitive and resistant isolates in cellular and colorectal explants ...
Clinical trial for Vertical infection transmission , Prevention of Perinatal Transmission of HIV-1 Without Nucleoside Reverse Transcriptase Inhibitors
Clinical trial for Vertical infection transmission , Prevention of Perinatal Transmission of HIV-1 Without Nucleoside Reverse Transcriptase Inhibitors
Racivir, also known as PSI-5004; (±)-FTC; RCV, 524W91, is a reverse transcriptase inhibitor potentially for the treatment of HIV infection. 524W91 was anabolized to the active 5-triphosphate in these cells. HBV replication was equally inhibited in cultures incubated with 524W91 when the drug was added 24 h preinfection, at infection, or 24 h postinfection. 524W91 inhibited HBV replication by 50% at less than 20 nM in human hepatocytes.
Learn more about Reverse Transcriptase Inhibitors at Memorial Hospital Coenzyme Q 10 - Possible Benefits and Risks St. Johns...
Learn more about Reverse Transcriptase Inhibitors at Memorial Hospital Coenzyme Q 10 - Possible Benefits and Risks St. Johns...
Learn more about Reverse Transcriptase Inhibitors at Doctors Hospital of Augusta Coenzyme Q 10 - Possible Benefits and Risks ...
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South Africa (SA) has the highest proportion of HIV-positive people in the world. In 2013, an estimated 10% of the population was HIV-positive, which amounted to 5.26 million people.[1] For adults between the ages of 15 and 49 years, an estimated 15.90% were HIV-positive.[1] However, SA has made positive changes in managing the HIV epidemic. The number of people on antiretroviral therapy (ART) has increased, and there have been fewer AIDS-related deaths from 2005 to 2011.[2]. Antiretrovirals used in the management of HIV. HIV cannot be cured; however, there are several major classes of drugs used in its management. The five classes of drugs used for the management of HIV are entry inhibitors, fusion inhibitors, integrase inhibitors, protease inhibitors and reverse transcriptase inhibitors (nucleoside reverse transcriptase inhibitors and non-nucleoside reverse transcriptase inhibitors).[3] These agents act through various mechanisms to stop the replication of HIV. The recommended regimens for the ...
Pronunciation guide (phonetic spelling and recorded audio) of emtricitabine; tenofovir; rilpivirine, also known as Complera, which is a Top 250 Drug in the drug class of Nucleoside reverse transcriptase inhibitor (NRTI); Non-nucleoside reverse transcriptase inhibitor (NNRTI).
For patients who are starting to take antiretroviral medication (to treat HIV) for the first time, there are now a variety of different medicines which may be taken together as a combination in order to form an effective treatment which suppresses the virus for prolonged periods of time. Currently, national guidelines recommend the use of two different drugs of one type (the nucleoside/ nucleotide reverse transcriptase inhibitors, NRTI often known as nukes) with a third drug from one of two other types (either a nonnucleoside reverse transcriptase inhibitor, known as an NNRTI or nonnuke, or a protease inhibitor, known as a PI) to form a treatment regime of three active drugs. In the UK and Europe, all PIs are given in combination with a small dose of a second PI, ritonavir, which has the effect of boosting the levels of the active PI in the bloodstream. The investigators know from both research studies and patient experience in clinic that a combination of a ritonavirboosted PI with an NNRTI ...
The human immunodeficiency virus (HIV) causes AIDS (acquired immune deficiency syndrome), a disease in which the immune system progressively deteriorates, making sufferers vulnerable to all manner of opportunistic infections. Currently, world-wide there are estimated to be 34 million people living with HIV,
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Effect of a bound non-nucleoside RT inhibitor on the dynamics of wild-type and mutant HIV-1 reverse transcriptase.: HIV-1 reverse transcriptase (RT) is an impor
This study aims at identifying predictors of the treatment decision of German physicians with regard to a non-nucleoside reverse transcriptase inhibitor (NNRTI) or a ritonavir-boosted protease inhibitor (PI/r) -based initial treatment regimen. The study is based on a sub analysis of a nation-wide multi-centre, non-interventional, prospective cohort study. 133 patients were identified, who received antiretroviral first-line therapy. By means of a logistic regression, factors that determine the treatment strategy for treatment-naïve patients were analysed. Compared to patients receiving a NNRTI-based initial regimen, patients treated with PI/r are slightly younger, less educated, in a later stage of HIV and have more concomitant diseases. Regression analysis revealed that being in a later stage of HIV (CDC-C) is significantly associated with a PI/r-based treatment decision. Our analysis is the first study in Germany investigating sociodemographic and disease-specific parameters associated with a NNRTI-
ENGLISH ABSTRACT: Since its discovery in the 1980s, HIV has affected the lives of millions of individuals around the globe. Despite obvious need and an enormous amount of research a cure has remained elusive due to the rapid onset of mutated forms of the virus. However, there has been considerable success in reducing viral levels of infected individuals through the use of highly active antiretroviral therapy (HAART). The first-line regimen HAART mainly targets reverse transcriptase (RT) through the employment of two nucleoside RT inhibitors (NRTIs) and a nonnucleoside RT inhibitor (NNRTI). NNRTIs target an allosteric pocket situated about 10 Å from the catalytic site and cause a conformational change in the enzyme upon binding, leading to the inhibition of viral replication. There are currently 5 FDA approved NNRTIs on the market which successfully inhibit viral replication, but the use of these drugs is becoming limited due to the onset of drug resistant strains of the virus. In light of this ...
Nucleoside reverse transcriptase inhibitors (NRTIs) are mainstay therapeutics for HIV that block retrovirus replication. Alu (an endogenous retroelement that also requires reverse transcriptase for its life cycle)-derived RNAs activate P2X7 and the NLRP3 inflammasome to cause cell death of the retinal pigment epithelium in geographic atrophy, a type of age-related macular degeneration. We found that NRTIs inhibit P2X7-mediated NLRP3 inflammasome activation independent of reverse transcriptase inhibition. Multiple approved and clinically relevant NRTIs prevented caspase-1 activation, the effector of the NLRP3 inflammasome, induced by Alu RNA. NRTIs were efficacious in mouse models of geographic atrophy, choroidal neovascularization, graft-versus-host disease, and sterile liver inflammation. Our findings suggest that NRTIs are ripe for drug repurposing in P2X7-driven diseases ...
This nested case-control study examined relationships between MDR1, CYP2B6, and CYP3A4 variants and hepatotoxicity during antiretroviral therapy with either efavirenz- or nevirapine-containing regimens. Decreased risk of hepatotoxicity was associated with MDR1 3435C→;T (odds ratio, 0.254; P = .021). An interaction between MDR1 and hepatitis B surface antigen status predicted risk with 82% accuracy (P , .001).. ...
SUSTIVA® (sus-TEE-vah) [efavirenz (eh-FAH-vih-rehnz)] capsules and tablets. ALERT: Find out about medicines that should NOT be taken with SUSTIVA.. Please also read the section MEDICINES YOU SHOULD NOT TAKE WITH SUSTIVA.. Read this information before you start taking SUSTIVA (efavirenz). Read it again each time you refill your prescription, in case there is any new information. This leaflet provides a summary about SUSTIVA and does not include everything there is to know about your medicine. This information is not meant to take the place of talking with your doctor.. What is SUSTIVA?. SUSTIVA is a medicine used in combination with other medicines to help treat infection with Human Immunodeficiency Virus type 1(HIV-1), the virus that causes AIDS (acquired immune deficiency syndrome). SUSTIVA is a type of anti-HIV drug called a non-nucleoside reverse transcriptase inhibitor (NNRTI). NNRTIs are not used in the treatment of Human Immunodeficiency Virus type 2 (HIV-2) infection.. SUSTIVA ...
Virtually all the compounds that are currently used, or under advanced clinical trial, for the treatment of HIV infections, belong to one of the following classes: (i) nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs): i.e., zidovudine (AZT), didanosine (ddI), zalcitabine (ddC), stavudine (d4T), lamivudine (3TC), abacavir (ABC), emtricitabine [(-)FTC], tenofovir (PMPA) disoproxil fumarate (ii) non-nucleoside reverse transcriptase inhibitors (NNRTIs): i.e., nevirapine, delavirdine, efavirenz, emivirine (MKC- 442) and (iii) protease inhibitors (PIs): i.e., saquinavir, ritonavir, indinavir, nelfinavir, amprenavir, and lopinavir. In addition to the reverse transcriptase and protease step, various other events in the HIV replicative cycle are potential targets for chemotherapeutic intervention: (i) viral adsorption, through binding to the viral envelope glycoprotein gp120 (polysulfates, polysulfonates, polyoxometalates, zintevir, negatively charged albumins, cosalane analogues) (ii) ...
Anti-HIV drug treatment. Whilst the number of people living with HIV is rising each year, the number of HIV infections that progress to AIDS has dropped dramatically since 1996. This is primarily the result of anti-retroviral therapies, which are available to slow the progress of the virus.. Antiretroviral drugs (ARVs) target essential components of the viral replication cycle and include reverse transciptase (RT) inhibitors, which interfere with the way the virus makes a complementary cDNA copy of its RNA genome, and protease inhibitors, which prevent the virus from cutting up the raw materials it needs to form new viral particles.. Drugs that block RT fall into two categories. These are known as nucleoside and non-nucleoside RT inhibitors. The nucleoside RT inhibitors are structurally very similar to normal DNA bases, but they lack a critical chemical group required to enable a DNA chain to grow. So when the viral RT inserts one of these altered bases into the copy that its making of its ...
Discovery and development of nucleoside and nucleotide reverse-transcriptase inhibitors (NRTIs and NtRTIs) began in the 1980s when the AIDS epidemic hit Western societies. NRTIs inhibit the reverse transcriptase (RT), an enzyme that controls the replication of the genetic material of the human immunodeficiency virus (HIV). The first NRTI was zidovudine, approved by the U.S. Food and Drug Administration (FDA) in 1987, which was the first step towards treatment of HIV. Six NRTI agents and one NtRTI have followed. The NRTIs and the NtRTI are analogues of endogenous 2´-deoxy-nucleoside and nucleotide. Drug-resistant viruses are an inevitable consequence of prolonged exposure of HIV-1 to anti-HIV drugs. In the summer of 1981 the acquired immunodeficiency syndrome (AIDS) was first reported. Two years later the etiological link to AIDS, the human immunodeficiency virus (HIV) was identified. Since the identification of HIV the development of effective antiretroviral drugs and the scientific ...
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Upon prolonged treatment with various antiretroviral nucleoside analogs such as 3-azido-3-deoxythymidine, 2,3-dideoxyinosine, 2,3-dideoxycytidine, (-)- beta-L-2, 3dideoxy-3thiacytidine and 2,3-didehydro-3-deoxythymidine, selection of human immunodeficiency virus type 1 (HIV-1) strains with mutations in the reverse transcriptase (RT) gene has been reported. We designed a reverse hybridization line probe assay (LiPA) for the rapid and simultaneous characterization of the following variations in the RT gene: M41 or L41; T69, N69, A69, or D69; K70 or R70; L74 or V74; V75 or T75; M184, I184, or V184; T215, Y215, or F215; and K219, Q219, or E219. Nucleotide polymorphisms for codon L41 (TTG or CTG), T69 (ACT or ACA), V75 (GTA or GTG), T215 (ACC or ACT), and Y215 (TAC or TAT) could be detected. In addition to the codons mentioned above, several third-letter polymorphisms in the direct vicinity of the target codons (E40, E42, K43, K73, D76, Q182, Y183, D185, G213, F214, and L214) were found, ...
Nonnucleoside opposite transcriptase (RT) inhibitors (NNRTI) and integrase (IN) strand transfer inhibitors (INSTI) are fundamental the different parts of antiretroviral regimens. of raltegravir (RAL); the RT-K103N mutation experienced no impact. The NNRTI level of resistance mutations experienced no influence on RAL susceptibility. Similarly, the IN-G140S/Q148H mutations experienced no influence on EFV or RPV susceptibility. Nevertheless, both RT-K103N plus IN-G140S/Q148H as well as the RT-E138K plus IN-G140S/Q148H mutant infections experienced significantly greater collapse raises in 50% inhibitory focus (IC50) of EFV than infections carrying an individual NNRTI mutation. Similarly, the RT-E138K plus IN-G140S/Q148H mutant computer virus experienced significantly greater collapse raises in RAL IC50 than that of the IN-G140S/Q148H mutant computer virus. These results claim that relationships between RT and IN mutations IL12RB2 are essential for NNRTI and INSTI level of resistance and viral ...
SUSTIVA® (sus-TEE-vah) [efavirenz (eh-FAH-vih-rehnz)] capsules and tablets. ALERT: Find out about medicines that should NOT be taken with SUSTIVA.. Please also read the section MEDICINES YOU SHOULD NOT TAKE WITH SUSTIVA.. Read this information before you start taking SUSTIVA (efavirenz). Read it again each time you refill your prescription, in case there is any new information. This leaflet provides a summary about SUSTIVA and does not include everything there is to know about your medicine. This information is not meant to take the place of talking with your doctor.. What is SUSTIVA?. SUSTIVA is a medicine used in combination with other medicines to help treat infection with Human Immunodeficiency Virus type 1(HIV-1), the virus that causes AIDS (acquired immune deficiency syndrome). SUSTIVA is a type of anti-HIV drug called a non-nucleoside reverse transcriptase inhibitor (NNRTI). NNRTIs are not used in the treatment of Human Immunodeficiency Virus type 2 (HIV-2) infection.. SUSTIVA ...
Nonnucleoside slow transcriptase inhibitors (NNRTIs) target HIV-1 slow transcriptase (RT) by binding to a pocket in RT thats near, but distinct, through the DNA polymerase energetic site and stop the formation of viral cDNA. set up and demonstrate that legislation of Gag-Pol/Gag-Pol connections is a book target for little molecule inhibitors of HIV-1 creation. Furthermore, these medications can serve as useful probes to help expand understand processes involved with HIV-1 particle set up and maturation. Synopsis HIV-1 encodes invert transcriptase (RT), an enzyme thats essential for computer virus replication. Nonnucleoside invert transcriptase inhibitors (NNRTIs) are allosteric inhibitors from the HIV-1 RT. In HIV-1-contaminated cells NNRTIs stop the RT-catalyzed synthesis of the double-stranded DNA duplicate from the viral genomic RNA, which can be an early part of the computer virus life cycle. Powerful NNRTIs possess the book feature of marketing the interaction between your two RT ...
One of the major problems for AIDS control is the ability of HIV‐1 to develop resistance to antiretroviral compounds used individually or in combination (Balzarini, 1999 and references therein). Sequential monotherapy or combination therapy with several nucleoside RT inhibitors can lead to the appearance of multidrug‐resistant strains. These isolates can accumulate resistance mutations specific for AZT (e.g. M41L, D67N, L210W or T215Y) and other RT inhibitors (e.g. K65R for ddC, L74V for ddI, etc.), which arise during monotherapy. Alternatively, multidrug‐resistant HIV‐1 strains containing the amino acid substitutions A62V, V75I, F77L, F116Y and Q151M may appear under combination therapy with nucleoside RT inhibitors (Shirasaka et al., 1995). Recently, a different multidrug resistance pattern of amino acid substitutions has been observed in a number of patients who were exposed to AZT, ddI, ddC and/or d4T in prolonged therapeutic regimens. Substitution of Thr69 by Ser and insertion of ...
This is a 96 week study to determine if UK- 453,061 in combination with Darunavir /ritonavir and a Nucleos(t)ide Reverse Transcriptase inhibitor is as efficacious, safe and tolerable as etravirine in combination with Darunavir /ritonavir and a Nucleos(t)ide Reverse Transcriptase inhibitor in HIV-1 infected patients who have been previously treated with antiretroviral drugs and have NNRTI resistance mutations ...
Zidovudine (Retrovir). The human immunodeficiency virus replicates by converting its single-standed RNA into double-stranded DNA which is incorporated into host DNA; this crucial conversion, the reverse of the normal cellular transcription of nucleic acids, is accomplished by the enzyme reverse transcriptase. Zidovudine, as the triphosphate, was the first anti-HIV drug to be introduced and has a high affinity for reverse transcriptase. It is integrated by it into the viral DNA chain, causing premature chain termination. The drug must be present continuously to prevent viral alteration of the host DNA, which is permanent once it occurs.. Pharmacokinetics. Zidovudine is well absorbed from the gastrointestinal tract (it is available as capsules and syrup) and is rapidly cleared from the plasma (t1/^ 1 h); concentrations in CSF are approximately half those in plasma. It is also available i.v. for patients temporarily unable to take oral medications. The drug is mainly metabolically inactivated, but ...
TY - JOUR. T1 - Erratum. T2 - Combination nucleoside/nucleotide reverse transcriptase inhibitors for treatment of HIV infection (Expert Opinion on Pharmacotherapy (2012) 13:1(65-79)). AU - Akanbi, M. O.. AU - Scarsi, Kimberly K. AU - Taiwo, B.. AU - Murphy, R. L.. PY - 2015/5/1. Y1 - 2015/5/1. UR - http://www.scopus.com/inward/record.url?scp=84928534685&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=84928534685&partnerID=8YFLogxK. U2 - 10.1517/14656566.2015.1039789. DO - 10.1517/14656566.2015.1039789. M3 - Comment/debate. C2 - 25887247. AN - SCOPUS:84928534685. VL - 16. JO - Expert Opinion on Pharmacotherapy. JF - Expert Opinion on Pharmacotherapy. SN - 1465-6566. IS - 7. ER - ...
A novel HIV-1 inhibitor, 6-(tert-butyl)-4-phenyl-4-(trifluoromethyl)-1H,3H-1,3,5-triazin-2-one (compound 1), was identified from a compound library screened for the ability to inhibit HIV-1 replication. EC50 values of compound 1 were found to range from 107.9 to 145.4 nm against primary HIV-1 clinical isolates. In in vitro assays, HIV-1 reverse transcriptase (RT) activity was inhibited by compound 1 with an EC50 of 4.3 μm. An assay for resistance to compound 1 selected a variant of HIV-1 with a RT mutation (RT(L100I) ); this frequently identified mutation confers mild resistance to non-nucleoside RT inhibitors (NNRTIs). A recombinant HIV-1 bearing RT(L100I) exhibited a 41-fold greater resistance to compound 1 than the wild-type virus. Compound 1 was also effective against HIV-1 with RT(K103N) , one of the major mutations that confers substantial resistance to NNRTIs. Computer-assisted docking simulations indicated that compound 1 binds to the RT NNRTI binding pocket in a manner similar to that ...
Three types of antiretroviral drugs (ARVs) are now used for the treatment of human immunodeficiency virus type 1 (HIV-1) infections, but only reverse transcriptase (RT) inhibitors are readily available to the vast majority of HIV-1-infected individuals in the developing world. The treatment regimen of choice is a combination of a nonnucleoside RT inhibitor (almost exclusively nevirapine [NVP]) and two nucleoside RT inhibitors, i.e., zidovudine (AZT) or stavudine plus lamivudine or didanosine.. In addition to being the backbone of most treatment regimens, NVP is provided as a single dose to block the mother-to-child transmission (MTCT) of HIV-1 in developing countries. In the absence of antiretroviral therapy, the frequency of MTCT is approximately 25 to 48% (2, 36, 38), whereas the administration of a short course of AZT therapy near the end of gestation (7, 8, 49) or the administration of a single dose of NVP at labor can reduce the rate of perinatal transmission to less than 20% (22, 25, 32, ...
FOSTER CITY, Calif. & WHITEHOUSE STATION, N.J.--(BUSINESS WIRE)--Aug. 11, 2006--Gilead Sciences, Inc. (Nasdaq: GILD) and Merck & Co., Inc. (NYSE: MRK) today announced that the companies have established an agreement for the distribution of ATRIPLA(TM) (efavirenz 600 mg/ emtricitabine 200 mg/ tenofovir disoproxil fumarate 300 mg), a once-daily, single tablet regimen for the treatment of HIV-1 infection in adults, in developing countries around the world.. ATRIPLA contains 600 mg of efavirenz, a non-nucleoside reverse transcriptase inhibitor (NNRTI), 200 mg of emtricitabine and 300 mg of tenofovir disoproxil fumarate, both nucleoside reverse transcriptase inhibitors (NRTIs). Efavirenz is marketed by Merck under the tradename Stocrin(R) in all territories outside of the United States, Canada and certain European countries (where it is commercialized by Bristol-Myers Squibb under the tradename Sustiva(R)). Emtricitabine and tenofovir disoproxil fumarate are commercialized by Gilead Sciences under ...
The prices of reverse transcriptase (RT) inhibitors in Thailand have been reduced since December 1, 2001. It is expected that reduction in the price of these inhibitors may influence the drug resistance mutation pattern of HIV-1 among infected people. This study reports the frequency of HIV-1 genetic mutation associated with drug resistance in antiretroviral-treated patients from Thailand. Genotypic resistance testing was performed on samples collected in 2002 from 88 HIV-1 infected individuals. Automated DNA sequencing was used to genotype the HIV-1 polymerase gene isolated from patients plasma. Resistance to protease inhibitors, nucleoside and non-nucleoside reverse transcriptase inhibitors were found in 10 (12%), 42 (48%) and 19 (21%) patients, respectively. The most common drug resistance mutations in the protease gene were at codon 82 (8%), 90 (7%) and 54 (6%), whereas resistant mutations at codon 215 (45%), 67 (40%), 41 (38%) and 184 (27%) were commonly found in the RT gene. This finding
Effect of Food on Absorption of Abacavir and lamivudine Abacavir and lamivudine may be administered with or without food. Administration with a high-fat meal in a single-dose bioavailability trial resulted in no change in AUClast, AUC∞, and Cmax for lamivudine. Food did not alter the extent of systemic exposure to abacavir (AUC∞), but the rate of absorption (Cmax) was decreased approximately 24% compared with fasted conditions (n = 25). These results are similar to those from previous trials of the effect of food on abacavir and lamivudine tablets administered separately.. Specific Populations Patients with Renal Impairment: Abacavir and lamivudine: The effect of renal impairment on the combination of abacavir and lamivudine has not been evaluated (see the U.S. prescribing information for the individual abacavir and lamivudine components).. Patients with Hepatic Impairment: Abacavir and lamivudine: The effect of hepatic impairment on the combination of abacavir and lamivudine has not been ...
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In previously untreated patients, combinations that include efavirenz compare favorably with regimens that include either other nonnucleoside reverse transcriptase inhibitors or components from other antiretroviral classes.. Two parallel randomized, placebo-controlled Phase III studies in antiretroviral-naive adults compared efavirenz with rilpivirine, each in combination with 2 NRTIs (predominantly tenofovir + emtricitabine). By ITT analysis of pooled data from the 2 studies, 82% of efavirenz recipients and 84% of rilpivirine recipients had HIV RNA levels of ,50 copies/mL at 48 weeks; the difference was not statistically significant. In patients with HIV RNA ,100,000 copies/mL, the efavirenz regimen resulted in higher rates of virologic suppression. The mean increase in CD4 count was 176 cells/µL in the efavirenz group (compared with 192 cells/µL in the rilpivirine group).(13) A randomized trial comparing efavirenz with nevirapine, each given with lamivudine + stavudine in initial therapy, ...
Globally of today, acquired immunodeficiency syndrome (AIDS) and malaria are two of the most threatening diseases known to mankind. The World Health Organization estimated that AIDS and malaria together claimed nearly 4 million lives in 2003 and many more were infected by the causative agent human immunodeficiency virus (HIV) and the Plasmodium falciparum (P. falicparum) parasite. Current treatment regims for HIV and P. falicparum infections are undermined by rapid emergence of drug-resistant strains and severe drug side-effects.. A resistance mechanism of the commonly selected K103N RT mutant towards three second generation non-nucleoside RT inhibitors (NNRTIs) is presented based on X-ray structures. Subtle changes in contacts between inhibitor and residue in position 103 aided the design of improved inhibitors. For the PR target, attempts have been made to structurally assist the development of diol-based protease inhibitors (PIs) with the aim of improving the anti-viral potency without ...
Antiretroviral drugs are a very effective therapy against HIV infection. However, the high mutation rate of HIV permits the emergence of variants that can be resistant to the drug treatment. Predicting drug resistance to previously unobserved variants is therefore very important for an optimum medical treatment. In this paper, we propose the use of weighted categorical kernel functions to predict drug resistance from virus sequence data. These kernel functions are very simple to implement and are able to take into account HIV data particularities, such as allele mixtures, and to weigh the different importance of each protein residue, as it is known that not all positions contribute equally to the resistance. We analyzed 21 drugs of four classes: protease inhibitors (PI), integrase inhibitors (INI), nucleoside reverse transcriptase inhibitors (NRTI) and non-nucleoside reverse transcriptase inhibitors (NNRTI). We compared two categorical kernel functions, Overlap and Jaccard, against two well-known
Nevirapine is a non-nucleoside reverse transcriptase inhibitor used to reduce the viral load in HIV infection. Its side effects include hepatotoxicity, gastrointestinal symptoms, and dermatological reaction.1 Efiravenz, another non-nucleoside reverse transcriptase inhibitor, has a similar structure to nevirapine and can cause insomnia and psychotic reactions.1 We report three cases of neuropsychiatric sequelae to nevirapine in patients with HIV infection but no history of mental illness. Medline, Embase, and PsychLIT list no reported cases.. Within two weeks of starting nevirapine a 35 year old man developed low mood and had to stop working because of cognitive impairment and clouding of consciousness. He was admitted after taking an overdose of nevirapine and the treatment was stopped. Five days later, fearing that nursing staff would kill him, he leapt through a third floor window. As the temporal connection to his deterioration was unclear, nevirapine treatment was restarted. After a two week ...
HIV causes a person to become more prone to illness, so infected people need treatment options. However, there is no cure for HIV. To help ease negative symptoms, drugs called anti-retroviral therapy (ART) are available. This treatment is also called high active anti-retroviral therapy (HAART). HAART treatment begins with one non-nucleoside reverse transcriptase inhibitor (NNRTI) and two nucleoside analogue reverse transcriptase inhibitors (NRTIs).[2] The NRTI drug could be named zidovudine (AZT), tenofovir (TDF), andlamivudine (3TC), or emtricitabine (FTC).[3] These drugs slow the progression of the HIV virus in the body.[3] Usually, these treatments consist of a combination of three or more drugs, and each drug performs a different job in fighting the virus. In general, HAART prevents the HIV from multiplying and destroying CD4 cells. CD4 cells are necessary to help protect the body from infections and cancer.[4] Since the HIV virus destroys CD4 cells, it causes people with HIV to be more ...
The introduction of antiretroviral therapy (ART) has intensely reduced HIV-1 associated deaths, mother-to-child HIV-1 transmission, and adult HIV-1 rates. This is as a result of the extensive administration of homogeneous first line regimens that contain two nucleoside reverse transcriptase inhibitors commonly referred to as NRTIs as well as a nonnucleoside RT inhibitor referred to as NNRT. Unfortunately, the long-term success of ART is affected by the development of acquired drug resistance (ADR) and transmitted drug resistance (TDR).. There is an increasing popularity of acquired and transmitted HIV-1 drug resistance. This has consequently become a major obstacle to the success of antiretroviral therapy in the low and middle-income countries that have been hit hardest by the HIV-1 epidemic. To address this issue, experts recommend genotypic drug resistance testing to facilitate the choice of initial ART in areas where there is an increase in transmitted drug resistance. This will also enable ...
Calanolide A is a new non-nucleoside reverse transcriptase inhibitor (NNRTI) derived from a plant found in the Malaysian rain forest. A related compound, calanolide B, also has anti-HIV activity. Both drugs are being developed by Sarawak Pharmaceuticals. A preliminary dosing study among HIV-infected individuals showed a significant antiviral effect compared with placebo.
Emtricitabine is a nucleoside reverse transcriptase inhibitor with an IC50 of 27.7 μM. Buy Reverse Transcriptase inhibitor Emtricitabine from AbMole BioScience.
Etravirine (ETR,[1] brand name Intelence, formerly known as TMC125) is a drug used for the treatment of HIV. Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). Unlike the currently available agents in the class, resistance to other NNRTIs does not seem to confer resistance to etravirine.[2] Etravirine is marketed by Tibotec, a subsidiary of Johnson & Johnson. In January 2008, the Food and Drug Administration approved its use for patients with established resistance to other drugs, making it the 30th anti-HIV drug approved in the United States and the first to be approved in 2008.[3] It was also approved for use in Canada on April 1, 2008.[4]. Etravirine is licensed in the United States, Canada, Israel, Russia, Australia and the European Union,[5] and is under regulatory review in Switzerland.[6]. ...
TY - JOUR. T1 - Creation of a long-acting nanoformulated 29,39-dideoxy-39-thiacytidine. AU - Guo, Dongwei. AU - Zhou, Tian. AU - Araínga, Mariluz. AU - Palandri, Diana. AU - Gautam, Nagsen. AU - Bronich, Tatiana K. AU - Alnouti, Yazen. AU - McMillan, JoEllyn M. AU - Edagwa, Benson J. AU - Gendelman, Howard Eliot. PY - 2017/3/1. Y1 - 2017/3/1. N2 - Background: Antiretroviral drug discovery and formulation design will facilitate viral clearance in infectious reservoirs. Although progress has been realized for selected hydrophobic integrase and nonnucleoside reverse transcriptase inhibitors, limited success has been seen to date with hydrophilic nucleosides. To overcome these limitations, hydrophobic long-acting drug nanoparticles were created for the commonly used nucleoside reverse transcriptase inhibitor, lamivudine (29,39-dideoxy-39-thiacytidine, 3TC). Methods: A 2-step synthesis created a slow-release long-acting hydrophobic 3TC. Conjugation of 3TC to a fatty acid created a myristoylated ...
One approach that has been used to combat HIV-1 infection is the use of ART, or antiretroviral therapy, and this approach has proven to be effective at reducing viral levels in the blood. ART suppresses HIV-1 viremia to undetectable levels within 12-48 weeks in a majority of patients. This therapy is a cocktail or combination therapy of three or more drugs, including 2 nucleoside-based reverse transcriptase inhibitors (prevents production of the virus genome by inhibiting RNAàDNA transcription), and one or more of the following drugs: non-nucleoside reverse transcriptase inhibitors, membrane fusion inhibitors, viral protease inhibitors, or integrase inhibitors. Each of these drugs targets a specific part of the viral lifecycle, making it unable to replicate and infect other cells. Because each drug is mutually exclusive and targets a different area of the lifecycle, it is unlikely that a virus will develop resistance to all three drugs. Therefore, because the virus does not produce escape ...
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Objective: A novel rapid reverse transcriptase (RT) recombinant HIV-1 drug-susceptibility assay was developed to evaluate resistance to RT inhibitors.. Material and methods: HIV-1 RTs from five treatment-naive and 10 highly active antiretroviral therapy-experienced patients were evaluated. HIV-1 isolates recovered by culturing peripheral blood mononuclear cells from patients were used in the conventional isolate phenotype analysis. Recombinant HIV-1 strains were obtained by cloning the RT gene amplified from the supernatant of HIV-1 cultures in a plasmid carrying the HIV-1 strain HXB2 backbone, and the most represented clone for each virus isolate was then tested for antiviral drug susceptibility in parallel with HIV-1 isolates.. Results: Comparison of conventional virus isolate and the novel recombinant virus phenotypic assays showed a large concordance of results. However, some discrepant results were observed, in that higher drug-resistance levels were detected by the conventional isolate ...
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Anti-viral drug : A Coggle Diagram about ANTI HIV DRUGS (Protease Inhibitors, Nucleoside Reverse Transcriptase Inhibitors, Integrase inhibitor, Entry Inhibitors and Non Nucleoside Reverse Transcriptase Inhibitors) and ANTI HSV DRUGS (Ganciclovir and Acyclovir)
The public health approach to identify antiretroviral therapy failure: High-level nucleoside reverse transcriptase inhibitor resistance among Malawians failing first-line antiretroviral therapy ...
Bumpus has also researched nonnucleoside reverse transcriptase inhibitors. Her lab was the first to publish the P450-catalyzed ... Nucleotide Reverse Transcriptase Inhibitors". Expert Opinion on Pharmacotherapy. 13 (1): 65-79. doi:10.1517/14656566.2012. ... Tenofovir is a nucleotide analog reverse transcriptase inhibitor that prevents the HIV virus from replicating. Tenofovir is ... rilpivirine and etravirine and was first to characterize the metabolism of the nonnucleoside reverse transcriptase inhibitor ...
Montessori V, Harris M, Montaner JS (2003). "Hepatotoxicity of nucleoside reverse transcriptase inhibitors". Seminars in Liver ... including nucleoside reverse transcriptase inhibitors used to treat HIV, and a rare condition known as Jamaican vomiting ...
... such as a protease inhibitor, non-nucleoside reverse-transcriptase inhibitor, or integrase inhibitor; this type of therapy is ... ZDV is of the nucleoside analog reverse-transcriptase inhibitor (NRTI) class. It works by inhibiting the enzyme reverse ... Their research efforts were focused in part on the viral enzyme reverse transcriptase. Reverse transcriptase is an enzyme that ... Quan, Y; Rong, L; Liang, C; Wainberg, MA (1999). "Reverse Transcriptase Inhibitors Can Selectively Block the Synthesis of ...
It is of the reverse-transcriptase inhibitor class. Didanosine was first described in 1975 and approved for use in the United ... Like other anti-HIV nucleoside analogs, it acts as a chain terminator by incorporation and inhibits viral reverse transcriptase ...
Olivero, Ofelia A. (April 2007). "Mechanisms of genotoxicity of nucleoside reverse transcriptase inhibitors". Environmental and ...
It is a non-nucleoside reverse transcriptase inhibitor. While emivirine showed promising antiviral activity in vitro, it failed ...
Reverse-transcriptase. inhibitors (RTIs). Nucleoside and. nucleotide (NRTI). *Nucleoside analogues/NRTIs: Abacavir (ABC)°# ... Dolutegravir is an HIV integrase strand transfer inhibitor which blocks the functioning of HIV integrase which is needed for ... who are treatment-naïve or treatment-experienced but have not previously taken other integrase strand transfer inhibitors.[8] ... including those who have been treated with other integrase strand transfer inhibitors. Tivicay is also approved for children ...
Reverse-transcriptase. inhibitors (RTIs). Nucleoside and. nucleotide (NRTI). *Nucleoside analogues/NRTIs: Abacavir (ABC)°# ...
... is a non-nucleoside reverse transcriptase inhibitor (NNRTI). Unlike the currently available agents in the class, ... Etravirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI), designed to be active against HIV ... who have evidence of viral replication and HIV-1 strains resistant to a non-nucleoside reverse transcriptase inhibitor (NNRTI) ... and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug- ...
Lamivudine and abacavir are both nucleoside reverse transcriptase inhibitors (NRTI).[1] Abacavir/lamivudine was approved for ... Nucleotide analogue reverse transcriptase inhibitor. Lamivudine. Nucleotide analogue reverse transcriptase inhibitor. Clinical ... Reverse-transcriptase. inhibitors (RTIs). Nucleoside and. nucleotide (NRTI). *Nucleoside analogues/NRTIs: Abacavir (ABC)°# ...
Reverse-transcriptase. inhibitors (RTIs). Nucleoside and. nucleotide (NRTI). *Nucleoside analogues/NRTIs: Abacavir (ABC)°# ...
... (MK-1439) is a non-nucleoside reverse transcriptase inhibitor developed by Merck & Co. for use in the treatment of ... Reverse-transcriptase. inhibitors (RTIs). Nucleoside and. nucleotide (NRTI). *Nucleoside analogues/NRTIs: Abacavir (ABC)°# ...
It is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and ... Patients Comparing TMC278 to Efavirenz in Combination With 2 Nucleoside/Nucleotide Reverse Transcriptase Inhibitors". ... It is contraindicated for use with proton pump inhibitors due to the increased gastric pH causing decreased rilpivirine plasma ... Reverse-transcriptase. inhibitors (RTIs). Nucleoside and. nucleotide (NRTI). *Nucleoside analogues/NRTIs: Abacavir (ABC)°# ...
"Nucleoside reverse transcriptase inhibitors (NRTIs or 'nukes') - HIV/AIDS". www.hiv.va.gov. Archived from the original on 9 ... Abacavir is a nucleoside reverse transcriptase inhibitor that inhibits viral replication. It is a guanosine analogue that is ... Similar to other nucleoside analog reverse-transcriptase inhibitors (NRTIs), abacavir is used together with other HIV ... a Potent Inhibitor of HIV Reverse Transcriptase". The Journal of Organic Chemistry. 61 (13): 4192-4193. doi:10.1021/jo960708p. ...
It is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and ... Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). When taken by mouth, rilpivirine reaches highest ... "Human Biotransformation of the Nonnucleoside Reverse Transcriptase Inhibitor Rilpivirine and a Cross-Species Metabolism ... has not developed resistance to certain class of anti-HIV medicines called non-nucleoside reverse transcriptase inhibitors ( ...
Reverse-transcriptase. inhibitors (RTIs). Nucleoside and. nucleotide (NRTI). *Nucleoside analogues/NRTIs: Abacavir (ABC)°# ... Indinavir (IDV; trade name Crixivan, made by Merck) is a protease inhibitor used as a component of highly active antiretroviral ... Protease inhibitors changed the nature of AIDS from a terminal illness to a somewhat manageable one. It significantly increased ... Cohen J (June 1996). "Protease inhibitors: a tale of two companies". Science. 272 (5270): 1882-3. Bibcode:1996Sci...272.1882C. ...
... a reverse-transcriptase inhibitor used for HIV; cepharanthine, an alkaloid from stephania cepharantha hayata; and phosphonated ... "Susceptibility of Primary HTLV-1 Isolates from Patients with HTLV-1-Associated Myelopathy to Reverse Transcriptase Inhibitors ... HTLV-1 infection is thought to spread only through dividing cells since reverse transcriptase generates proviral DNA from ...
It belongs to the class of nucleoside reverse transcriptase inhibitors. KP-1461 is a prodrug of the active antiviral agent KP- ...
... is a nucleotide analog reverse-transcriptase inhibitor (NtRTI). It selectively inhibits viral reverse ... It is a nucleotide reverse transcriptase inhibitor and works by decreasing the ability of the viruses to replicate. Tenofovir ... the active compound that inhibits reverse transcriptase via chain termination. In fasting persons, bioavailability is 25%, and ... Tenofovir also interacts with HIV-1 protease inhibitors such as atazanavir, by decreasing atazanavir concentrations while ...
6.4.2.1 Nucleoside/nucleotide reverse transcriptase inhibitors. *6.4.2.2 Non-nucleoside reverse transcriptase inhibitors ...
... is a nucleoside analog reverse transcriptase translocation inhibitor that unlike other such inhibitors, inhibits HIV ... It is classified as a nucleoside reverse transcriptase translocation inhibitor (NRTTI). Merck is developing a subdermal drug- ... "The Crystal Structure of EFdA‐Resistant HIV‐1 Reverse Transcriptase Reveals Structural Changes in the Polymerase Active Site" ( ... Inhibits HIV-1 Reverse Transcriptase with Multiple Mechanisms". Journal of Biological Chemistry. 289 (35): 24533-48. doi: ...
It is an orally administered nucleotide analog reverse-transcriptase inhibitor (ntRTI). It can be formulated as the pivoxil ... Adefovir works by blocking reverse transcriptase, an enzyme crucial for the HBV to reproduce in the body. It is approved for ...
... is unique among non-nucleoside reverse transcriptase inhibitor (NNRTIs) in that it can bind to two distinct sites ... Calanolide A is an experimental non-nucleoside reverse transcriptase inhibitor (NNRTI). This compound was extracted from the ... on HIV reverse transcriptase enzyme. It may either bind to one or another site in the reverse transcriptase, but not both sites ... Naturally Occurring Nonnucleoside Reverse Transcriptase Inhibitor, in Healthy, Human Immunodeficiency Virus-Negative Human ...
... is a cytidine nucleoside analog and nucleoside reverse transcriptase inhibitor. It was found to inhibit HIV-1 ...
"Interface Peptides as Structure-based Human Immunodeficiency Virus Reverse Transcriptase Inhibitors". Journal of Biological ... Rittinger, K; Divita, G; Goody, R S (1995-08-15). "Human immunodeficiency virus reverse transcriptase substrate-induced ... Rittinger studied human immunodeficiency virus reverse transcriptase. At MRC National Institute for Medical Research Rittinger ... She has also collaborated with GlaxoSmithKline to discover inhibitors targeting the active site cysteine of thioester-forming ...
Menéndez-Arias L (June 2008). "Mechanisms of resistance to nucleoside analogue inhibitors of HIV-1 reverse transcriptase". ...
Trachtenberg, Joel D; Sande Merle A (July 2002). "Emerging resistance to nonnucleoside reverse transcriptase inhibitors: a ...
... is in the nucleoside reverse transcriptase inhibitors (NRTIs) family of medications. It prevents the hepatitis B ... virus from multiplying by blocking reverse transcriptase. Entecavir was approved for medical use in 2005. It is on the World ... proven more selective potent inhibitor of HBV by virtue of being Guanine NA 1998: Inhibition of hepadnaviral polymerases was ... "Identification of BMS-200475 as a Potent and Selective Inhibitor of Hepatitis B Virus". Antimicrob Agents Chemother. 41 (7): ...
Ateviridine is a non-nucleoside reverse transcriptase inhibitor that has been studied for the treatment of HIV. Preparation of ... 1. A Novel Class of Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors". Journal of Medicinal Chemistry. 37 (7): 999-1014. ... amine with the imidazolide derivative of 5-methoxy-3-indoleacetic acid produces the amide reverse transcriptase inhibitor, ...
Since zalcitabine is a reverse transcriptase inhibitor it possesses activity only against retroviruses. Zalcitabine has a very ... Zalcitabine (2′-3′-dideoxycytidine, ddC), also called dideoxycytidine, is a nucleoside analog reverse-transcriptase inhibitor ( ... This active metabolite works as a substrate for HIV reverse transcriptase, and also by incorporation into the viral DNA, hence ... was in practice prior to the second FDA approval and the triple drug combinations with dual NRTIs and a protease inhibitor (PI ...
Non-nucleoside reverse-transcriptase inhibitors. *NS5A inhibitors. *Nucleoside and nucleotide reverse-transcriptase inhibitors ...
is modified to include binding of the inhibitor to the free enzyme:. EI. +. S. ⇌. k. 3. k. −. 3. E. +. S. +. I. ⇌. k. −. 1. k. ... Reverse transcriptase. *Protein kinase *Tyrosine-kinase *Janus kinase. Hydrolase (EC 3). *3.1 Phosphodiesterase ... is the inhibitor concentration.. V. max. {\displaystyle V_{\max }}. remains the same because the presence of the inhibitor can ... To compute the concentration of competitive inhibitor [. I. ]. {\displaystyle {\ce {[I]}}}. that yields a fraction f. V. 0. {\ ...
... non-nucleoside reverse transcriptase inhibitors (NNRTI) - non-steroidal anti-inflammatory drugs (NSAID) - NRTI - nucleic acid ... nucleoside reverse transcriptase inhibitors (NRTI) - nucleotide - nucleotide analogs - nucleus - null cell ... reverse transcriptase - ribonucleic acid (RNA) - ribosome - RNA - route of administration - RT-PCR - RTI - Ryan White C.A.R.E. ... entry inhibitors - Env - envelope - enzyme - enzyme-linked immunosorbent assay (ELISA) - eosinophil - eosinophilic folliculitis ...
Industrial drugs that are designed as protease and reverse-transcriptase inhibitors are made such that they target specific ... the virus uses its own reverse transcriptase enzyme to produce DNA from its RNA genome, the reverse of the usual pattern, thus ... Virally encoded reverse transcriptase uses the pre-genomic RNA as a template for the creation of genomic DNA. ... Reverse transcriptase activity outside of retroviruses has been found in almost all eukaryotes, enabling the generation and ...
... following production of the double-stranded viral DNA by the viral RNA/DNA-dependent DNA polymerase reverse transcriptase. The ... In November 2005, data from a phase 2 study of an investigational HIV integrase inhibitor, MK-0518, demonstrated that the ... On October 12, 2007, the Food and Drug Administration (U.S.) approved the integrase inhibitor Raltegravir (MK-0518, brand name ... Antiretroviral effect of MK-0518, a novel HIV-1 integrase inhibitor, in ART-naïve HIV-1 infected patients. Program and ...
Non-nucleoside reverse-transcriptase inhibitors. *NS5A inhibitors. *Nucleoside and nucleotide reverse-transcriptase inhibitors ... NMDAR/TRPM4 interaction interface inhibitors (also known as ‚interface inhibitors') disrupt the NMDAR/TRPM4 complex and ... NMDAR inhibitors, including ketamine, esketamine (JNJ-54135419), rapastinel (GLYX-13), apimostinel (NRX-1074), 4- ... Huperzine A - a naturally occurring acetylcholinesterase inhibitor and potential antidementia agent. *Ibogaine - a naturally ...
Zinc finger inhibitors are typically used to combat HIV. HIV treatments usually rely on targeting reverse transcriptases and ... able to inhibit HIV-1 infection by inhibiting reverse transcription without an apparent impairment of reverse transcriptase. ... Zinc finger inhibitors, or zinc ejectors, are substances or compounds that interact adversely with zinc fingers and cause them ... NV038 is found to effect the function of the zinc finger after the virus has entered the cell but before reverse transcription ...
... using reverse transcriptase-a DNA polymerase that synthesizes a complementary DNA based on existing strands of RNA in a PCR- ... "DNA sequencing with chain-terminating inhibitors" in 1977.[21] Walter Gilbert and Allan Maxam at Harvard also developed ... of Sequencing by Hybridization and Cycle Sequencing for Genotyping of Human Immunodeficiency Virus Type 1 Reverse Transcriptase ... then detects the mRNA pieces using reverse transcription PCRs. The mRNA may then be amplified and sequenced. The combined ...
Chenyi Zhou, Liu Jinsong, Inhibition of human telomerase reverse transcriptase gene expression by BRCA1 in human ovarian cancer ... Direct interaction of c-Myc with Smad2 and Smad3 to inhibit TGF-beta-mediated induction of the CDK inhibitor p15(Ink4B), in Mol ... and c-Myc inhibits c-Myc-induced human telomerase reverse transcriptase gene (hTERT) promoter activity in breast cancer (PDF), ... K Gupta, Anand G, Yin X, Grove L, Prochownik E V, Mmip1: a novel leucine zipper protein that reverses the suppressive effects ...
Reverse transcriptase Telomerase. RNA nucleotidyltransferase. Template-directed. RNA polymerase I. II. III. IV. V. ssRNAP ... Pharmaceutical companies are designing and characterizing potential p110α isoform specific inhibitors.[14][15] ...
October 2005). "4-Phenylcoumarins as HIV transcription inhibitors". Bioorg. Med. Chem. Lett. 15 (20): 4447-50. doi:10.1016/j. ... Reverse transcriptase. *HIV-1 protease. *env *gp120. *gp41. VRAPs:. *transactivators *Tat. *Rev ...
... the reverse transcriptase enzyme of lentiviruses like HIV, SIV and FIV is typically dependent on Mg2+, whereas the analogous ... In acid soils Al3+ is a particularly strong inhibitor of Mg2+ uptake.[94][95] The inhibition by Al3+ and Mn2+ is more severe ...
Reverse transcriptase Telomerase. DNA nucleotidylexotransferase/Terminal deoxynucleotidyl transferase. RNA ...
Discovery and development of nucleoside and nucleotide reverse transcriptase inhibitors. *Discovery and development of Bcr-Abl ... Non-nucleoside reverse-transcriptase inhibitors. *NS5A inhibitors. *Nucleoside and nucleotide reverse-transcriptase inhibitors ... They induce apoptosis [63][64] and protein cascade via proteinase inhibitor,[63] have defense functions,[65] and regulate plant ... This approach is known as reverse pharmacology and is the most frequently used approach today.[17] ...
"Structure of HIV-2 reverse transcriptase at 2.35-A resolution and the mechanism of resistance to non-nucleoside inhibitors". ...
Zhou C, Liu J (March 2003). "Inhibition of human telomerase reverse transcriptase gene expression by BRCA1 in human ovarian ... "miR-182-mediated downregulation of BRCA1 impacts DNA repair and sensitivity to PARP inhibitors". Mol. Cell. 41 (2): 210-20. ... and c-Myc inhibits c-Myc-induced human telomerase reverse transcriptase gene (hTERT) promoter activity in breast cancer". J. ...
An example is the Merck and Dupont synthesis of Efavirenz, a potent HIV reverse transcriptase inhibitor. Lithium acetylide is ... However, the mechanism of how these additives reverse stereoselectivity is still being debated. There have been some challenges ...
... non-nucleoside reverse transcriptase inhibitor ବା NNRTI) ଓ ରିଭର୍ସ ଟ୍ରାନ୍ସକ୍ରିପ୍ଟେଜ (reverse transcriptase) କାମକୁ ଅବରୋଧ କରି ...
Reverse transcriptase Telomerase. RNA nucleotidyltransferase. Template-directed. RNA polymerase I. II. III. IV. V. ssRNAP ...
HIV-type 1 antiretroviral therapy agents like protease inhibitors and nonnucleoside reverse transcriptase inhibitors. ... "Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers".. *^ Goldsmith ME, Gudas JM, Schneider E ... For example, miR-27a up-regulates P-gp expression by suppressing Raf kinase inhibitor protein (RKIP);[27] alternatively, miR- ... Zhang H, Li M, Han Y, Hong L, Gong T, Sun L, Zheng X (September 2010). "Down-regulation of miR-27a might reverse multidrug ...
... nucleoside reverse transcriptase inhibitor) (NRTI) ଭାବରେ କାମକରେ ।[୧] ଯୁକ୍ତରାଷ୍ଟ୍ର ଆମେରିକାରେ ସନ ୨୦୦୪ରେ ଆବାକାଭିର/ଲାମିଭୁଡିନ ... Nucleotide analogue reverse transcriptase inhibitor. Lamivudine. Nucleotide analogue reverse transcriptase inhibitor. Clinical ...
Discovery and development of HIV-protease inhibitors. *Discovery and development of non-nucleoside reverse-transcriptase ...
Reverse transcriptase Telomerase. DNA nucleotidylexotransferase/Terminal deoxynucleotidyl transferase. RNA ...
Reverse transcriptase. *Protein kinase *Tyrosine-kinase *Janus kinase. Hydrolase (EC 3). *3.1 Phosphodiesterase ... of NSAID expenditures were for COX-2 inhibitors. Over the period of the study, COX-2 inhibitors rose from 10.03% of total ... "COX-2 Inhibitors and Cancer". Fact Sheet. United States National Cancer Institute. Archived from the original on May 9, 2008.. ... COX-2 inhibitors appear to work as well as nonselective NSAIDS.[5] They have not been compared to other treatment options such ...
... nucleoside/nucleotide reverse-transcriptase inhibitors (NRTIs/NtRTIs) and non-nucleoside reverse-transcriptase inhibitors ( ... Antiretroviral drug Reverse-transcriptase inhibitor Protease inhibitor Entry inhibitor Discovery and development of HIV- ... Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are antiretroviral drugs used in the treatment of human ... Jochmans D (June 2008). "Novel HIV-1 reverse transcriptase inhibitors". Virus Research. 134 (1-2): 171-85. doi:10.1016/j. ...
... active antiretroviral therapy regimens for controlling HIV/AIDS is still a combination of reverse transcriptase inhibitors ... In Reverse Transcriptase Inhibitors in HIV/AIDS Therapy, leading experts in AIDS/HIV drug discovery and development review all ... Comprehensive and up-to-date, Reverse Transcriptase Inhibitors in HIIV/AIDS Therapy offers a magisterial survey of the ... The authors synthesize our current understanding of the role of reverse transcriptase in the viral life cycle, describe the ...
Compare nucleoside reverse transcriptase inhibitors (NRTIs). View important safety information, ratings, user reviews, ... Nucleoside reverse transcriptase inhibitors (NRTIs). What are Nucleoside reverse transcriptase inhibitors (NRTIs)?. Nucleoside ... reverse transcriptase inhibitors (NRTIs) are active inhibitors of reverse transcriptase found in retroviruses such as the human ... List of Nucleoside reverse transcriptase inhibitors (NRTIs):. Filter by: -- all conditions --. Hepatitis B. HIV Infection. ...
Sequences matching input query are shown below. Original reference, patient identifier, isolate name, partial treatment histories and accession number are indicated. Complete treatment histories, when available, can be accessed by clicking the isolate name. Sequences may additionally be downloaded in the fasta format, or viewed as individual or composite alignments using the options above. If the user wishes to view individual alignments of isolates for which there are multiple clones, the user can choose to view either an alignment of consensus sequences derived from the clones or an alignment of each clone as well as a consensus sequence ...
... Reverse transcriptase inhibitors (RTIs) are a class of antiretroviral drug used to treat HIV ... Reverse transcriptase inhibitors - Phosphodiesterase inhibitors - Protease inhibitors (ACE inhibitor, Trypsin inhibitor). ... Nucleoside analog reverse transcriptase inhibitors (NARTIs or NRTIs) * Nucleotide analog reverse transcriptase inhibitors ( ... Non-nucleoside reverse transcriptase inhibitors (NNRTIs). Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are the ...
Nucleotide analog reverse-transcriptase inhibitors (NtARTIs or NtRTIs) Non-nucleoside reverse-transcriptase inhibitors (NNRTIs ... NNRTIs are therefore classified as non-competitive inhibitors of reverse transcriptase. Nucleoside analog reverse-transcriptase ... Discovery and development of non-nucleoside reverse-transcriptase inhibitors Protease inhibitors Discovery and development of ... Reverse-transcriptase inhibitors (RTIs) are a class of antiretroviral drugs used to treat HIV infection or AIDS, and in some ...
Non-nucleoside RT inhibitors. Non-nucleoside reverse transcriptase inhibitors (NNRTIs) interfere with reverse transcriptase by ... They are not competitive with nucleoside reverse transcriptase inhibitors as they work at a different site on the reverse ... RDEA806, a novel HIV non-nucleoside reverse transcriptase inhibitor, shows positive outcome in treatment of naive HIV patients ... of etravirine in the second-line antiretroviral therapy after failing an initial non-nucleoside reverse transcriptase inhibitor ...
Non-Nucleoside Reverse Transcriptase Inhibitors. Efavirenz (Sustiva, EFV). Last Updated: November 14, 2017; Last Reviewed: ...
Nucleoside reverse transcriptase inhibitors (NRTIs) stop HIV in its tracks by blocking reverse transcription, a process ... Nucleoside reverse transcriptase inhibitors possess intrinsic anti-inflammatory activity. By Benjamin J. Fowler, Bradley D. ... Nucleoside reverse transcriptase inhibitors possess intrinsic anti-inflammatory activity. By Benjamin J. Fowler, Bradley D. ... Nucleoside reverse transcriptase inhibitors possess intrinsic anti-inflammatory activity Message Subject. (Your Name) has ...
Learn more about Reverse Transcriptase Inhibitors at Portsmouth Regional Hospital Coenzyme Q 10 - Possible Benefits and Risks ... There are two major categories of reverse transcriptase inhibitors: nucleoside/nucleotide reverse transcriptase inhibitors ( ... non-nucleoside reverse transcriptase inhibitors (NNRTIs) . Reverse transcriptase inhibitors include: *Combivir (lamivudine and ... It does so by using an enzyme called reverse transcriptase. Reverse transcriptase inhibitors interfere with this process. ...
Learn more about Reverse Transcriptase Inhibitors at Medical City Dallas Coenzyme Q 10 - Possible Benefits and Risks St.... ... There are two major categories of reverse transcriptase inhibitors: nucleoside/nucleotide reverse transcriptase inhibitors ( ... non-nucleoside reverse transcriptase inhibitors (NNRTIs) . Reverse transcriptase inhibitors include: *Combivir (lamivudine and ... It does so by using an enzyme called reverse transcriptase. Reverse transcriptase inhibitors interfere with this process. ...
Nucleoside and Nucleotide Analogue Reverse Transcriptase Inhibitors. Emtricitabine (Emtriva, FTC). Last Updated: December 7, ...
Rational Design of Potent Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase. ... HIV-1 Reverse Transcriptase in complex with inhibitor GSK952. *DOI: 10.2210/pdb2yni/pdb ... REVERSE TRANSCRIPTASE/RIBONUCLEASE H A 563 Human immunodeficiency virus 1 EC#: 2.7.7.49 IUBMB 2.7.7.7 IUBMB 3.1.13.2 IUBMB 3.1. ...
Dapivirine (TMC120) is a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of ... Dapivirine (TMC120) is a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of ... Rilpivirine (R278474, TMC27, DB08864) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), and used to treat HIV-1 ... Tenofovir Alafenamide (GS-7340) is a prodrug of tenofovir, which is a reverse transcriptase inhibitor, used to treat HIV and ...
The mechanism of inhibition of HIV-1 reverse transcriptase by three nonnucleoside inhibitors is described. Nevirapine, O-TIBO, ... Mechanism of inhibition of HIV-1 reverse transcriptase by nonnucleoside inhibitors Science. 1995 Feb 17;267(5200):988-93. doi: ... The mechanism of inhibition of HIV-1 reverse transcriptase by three nonnucleoside inhibitors is described. Nevirapine, O-TIBO, ... of a nonnucleoside inhibitor and a nucleotide analog could bind very tightly and specifically to reverse transcriptase and ...
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity ...
What is reverse transcriptase inhibitor? Meaning of reverse transcriptase inhibitor as a legal term. What does reverse ... Definition of reverse transcriptase inhibitor in the Legal Dictionary - by Free online English dictionary and encyclopedia. ... Reverse transcriptase inhibitor legal definition of reverse transcriptase inhibitor https://legal-dictionary.thefreedictionary. ... inhibitor. (redirected from reverse transcriptase inhibitor). Also found in: Dictionary, Thesaurus, Medical, Acronyms, ...
... is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used to treat HIV-1 infection and AIDS. Find all the information ... Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI), and used to treat HIV-1 infection. ... Tenofovir Alafenamide (GS-7340) is a prodrug of tenofovir, which is a reverse transcriptase inhibitor, used to treat HIV and ... Lamivudine is a potent nucleoside analog reverse transcriptase inhibitor, used for treatment of chronic HBV and HIV/AIDS. It ...
Results suggesting associations with specific nucleoside reverse transcriptase inhibitor combinations need further ... This study did not evidence an overall increase in cancer risk in nucleoside reverse transcriptase inhibitor exposed children ... Incidence of cancer in children perinatally exposed to nucleoside reverse transcriptase inhibitors AIDS. 2008 Oct 18;22(16): ... Conclusion: This study did not evidence an overall increase in cancer risk in nucleoside reverse transcriptase inhibitor ...
Learn more about Reverse Transcriptase Inhibitors at Sky Ridge Medical Center Coenzyme Q 10 - Possible Benefits and Risks ... ... There are two major categories of reverse transcriptase inhibitors: nucleoside/nucleotide reverse transcriptase inhibitors ( ... non-nucleoside reverse transcriptase inhibitors (NNRTIs) . Reverse transcriptase inhibitors include: *Combivir (lamivudine and ... It does so by using an enzyme called reverse transcriptase. Reverse transcriptase inhibitors interfere with this process. ...
What is HIV? Get basic information on HIV, its symptoms, how it is spread, how HIV differs from AIDS, and how getting tested for HIV can help.. ...
Protease Inhibitors. HIV Protease Inhibitors. Reverse Transcriptase Inhibitors. Enzyme Inhibitors. Molecular Mechanisms of ... Observation of HIV-Infected Children Receiving Protease Inhibitor and Reverse Transcriptase Inhibitor. The safety and ... Currently on at least a three drug combination that includes a protease inhibitor (PI) and reverse transcriptase inhibitor (RTI ... or their medicines will be changed to a different combination of protease inhibitor and reverse transcriptase inhibitor. Before ...
... ... Several dual nucleoside reverse transcriptase inhibitor (NRTI) combinations provide efficacy when combined with a 3rd agent. ... Early nucleoside reverse transcriptase inhibitor (NRTI) backbone combinations improved upon the results seen with nucleoside ... However, there are a number of issues with current NRTI and nucleotide reverse transcriptase inhibitor (NtRTI) combinations ...
Nucleoside Reverse Transcriptase Inhibitor Combinations Nucleoside Reverse Transcriptase Inhibitor Combinations 24/05/2012 24/ ... Shah I. Nucleoside Reverse Transcriptase Inhibitor Combinations. Pediatr Oncall J. 2012;9: 56. doi: 10.7199/ped.oncall.2012.40 ... Shah I. Nucleoside Reverse Transcriptase Inhibitor Combinations. Pediatr Oncall J. 2012;9: 56. doi: 10.7199/ped.oncall.2012.40 ... Shah I. Nucleoside Reverse Transcriptase Inhibitor Combinations. Pediatr Oncall J. 2012;9: 56. doi: 10.7199/ped.oncall.2012.40 ...
Learn more about Reverse Transcriptase Inhibitors at JFK Medical Center Coenzyme Q 10 - Possible Benefits and Risks St. ... ... There are two major categories of reverse transcriptase inhibitors: nucleoside/nucleotide reverse transcriptase inhibitors ( ... non-nucleoside reverse transcriptase inhibitors (NNRTIs) . Reverse transcriptase inhibitors include: *Combivir (lamivudine and ... It does so by using an enzyme called reverse transcriptase. Reverse transcriptase inhibitors interfere with this process. ...
Non-nucleoside reverse transcriptase inhibitors (NNRTIs), their discovery, development, and use in the treatment of HIV-1 ... Reverse Transcriptase Inhibitors/history. *Reverse Transcriptase Inhibitors/pharmacology*. *Reverse Transcriptase Inhibitors/ ... their interaction with HIV-1 reverse transcriptase induces conformational changes that inhibit the catalytic activities of the ... It describes the characteristics of the NNRTIs, their mechanisms of action, HIV-1 resistance to the inhibitors, and the drugs ...
... delavirdine directly binds to reverse transcriptase and ... more ... non-nucleoside reverse-transcriptase inhibitor are used in the ... non-nucleoside reverse-transcriptase inhibitorNNRTIs inhibit viral replication.Delavirdine (Rescriptor)An NNRTI of HIV-1, ... encoded search term (Which medications in the drug class Antiretroviral agent%2C non-nucleoside reverse-transcriptase inhibitor ... non-nucleoside reverse-transcriptase inhibitor are used in the treatment of HIV Infection and AIDS? What to Read Next on ...
In search of a treatment for HIV--current therapies and the role of non-nucleoside reverse transcriptase inhibitors (NNRTIs).. ... Reverse Transcriptase Inhibitors/chemistry. *Reverse Transcriptase Inhibitors/pharmacology. *Reverse Transcriptase Inhibitors/ ... with specific emphasis on new developments within the class of allosteric non-nucleoside reverse transcriptase inhibitors ( ... HIV Reverse Transcriptase/antagonists & inhibitors*. *HIV Reverse Transcriptase/chemistry. *HIV Reverse Transcriptase/ ...
Figure 1. General structures of our recently reported triazole non-nucleoside reverse-transcriptase inhibitors (NNRTIs) [6] and ... Figure 1. General structures of our recently reported triazole non-nucleoside reverse-transcriptase inhibitors (NNRTIs) [6] and ... A Search for Dual Action HIV-1 Reverse Transcriptase, Bacterial RNA Polymerase Inhibitors ... Searching for novel scaffold of triazole non-nucleoside inhibitors ofHIV-1 reverse transcriptase. J. Enzym. Inhib. Med. Chem. ...
What is nucleoside reverse transcriptase inhibitor? Meaning of nucleoside reverse transcriptase inhibitor as a legal term. What ... does nucleoside reverse transcriptase inhibitor mean in law? ... Definition of nucleoside reverse transcriptase inhibitor in the ... protease inhibitors, non- nucleoside reverse transcriptase inhibitors, nucleoside/nucleotide reverse transcriptase inhibitors) ... Nucleoside reverse transcriptase inhibitor legal definition of nucleoside reverse transcriptase inhibitor https://legal- ...
  • There are two classes of drugs that target the HIV-1 RT enzyme, nucleoside/nucleotide reverse-transcriptase inhibitors (NRTIs/NtRTIs) and non-nucleoside reverse-transcriptase inhibitors (NNRTIs). (wikipedia.org)
  • RTIs come in three forms: Nucleoside analog reverse-transcriptase inhibitors (NARTIs or NRTIs) Nucleotide analog reverse-transcriptase inhibitors (NtARTIs or NtRTIs) Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) Nucleoside reverse transcriptase translocation inhibitor (NRTTIs). (wikipedia.org)
  • All NRTIs and NtRTIs are classified as competitive substrate inhibitors. (wikipedia.org)
  • NNRTIs are not incorporated into the viral DNA like NRTIs, but instead inhibit the movement of protein domains of reverse transcriptase that are needed to carry out the process of DNA synthesis. (wikipedia.org)
  • Nucleoside analog reverse-transcriptase inhibitors (NARTIs or NRTIs) compose the first class of antiretroviral drugs developed. (wikipedia.org)
  • Nucleoside reverse transcriptase inhibitors (NRTIs) are active inhibitors of reverse transcriptase found in retroviruses such as the human immunodeficiency virus ( HIV ). (drugs.com)
  • NNRTIs block reverse transcriptase by binding at a different site on the enzyme, compared to NRTIs and NtRTIs. (bionity.com)
  • Data are available from clinical trials in human pregnancy for the nucleoside reverse transcriptase inhibitors (NRTIs) zidovudine, abacavir, lamivudine, didanosine, emtricitabine, and stavudine and the nucleotide NRTI tenofovir disoproxil fumarate (TDF). (nih.gov)
  • It is quite likely that the child has developed resistance to the nucleoside reverse transcriptase inhibitors {NRTIs} in form of thymidine analog mutations {TAMs} which may cause resistance to other NRTI group. (pediatriconcall.com)
  • Newer drugs are selecting for different types of resistance, especially in nucleoside reverse transcriptase inhibitors (NRTIs), so that there may not be large numbers of thymidine analog mutations (TAMs) developing in patients who have started therapy in recent years. (thefreedictionary.com)
  • Surprisingly, support for this notion has come from testing the effect of removing single drugs from a failing regimen--in particular, nucleoside reverse transcriptase inhibitors (NRTIs). (thefreedictionary.com)
  • Each dose of Trizivir is a fixed-dose combination of Ziagen (abacavir/ABC), Retrovir (zidovudine/AZT), and Epivir (lamivudine/3TC), three nucleoside reverse transcriptase inhibitors (NRTIs) already approved by FDA. (thefreedictionary.com)
  • However, these 25 patients, all of whom were naive to non- nucleoside reverse transcriptase inhibitors (NNRTIs), were given efavirenz (Sustiva), a potent NNRTI, in addition to Kaletra and nucleoside reverse transcriptase inhibitors (NRTIs). (thefreedictionary.com)
  • The French have reported 8 cases of mitochondrial toxicity in uninfected infants with neonatal exposure to nucleoside reverse transcriptase inhibitors (NRTIs) who developed neurological and developmental abnormalities leading to 2 deaths. (thefreedictionary.com)
  • Usually one PI is combined with 2 nucleoside reverse transcriptase inhibitors (NRTIs), the first class of approved antiretroviral drugs. (thefreedictionary.com)
  • In treatment-experienced patients with HIV and viral resistance, optimized regimens that omitted nucleoside reverse transcriptase inhibitors (NRTIs) were shown to be as equally effective and safe as those that included these agents. (aphanet.org)
  • To evaluate the efficacy of nucleoside reverse transcriptase inhibitors (NRTIs) in the laser-induced mouse model of choroidal neovascularization (CNV). (arvojournals.org)
  • The purpose of the study reported here was to compare the antiviral efficacy against feline immunodeficiency virus (FIV) and cytotoxicity in feline peripheral blood mononuclear (PBM) cells of 9 nucleoside reverse transcriptase inhibitors (NRTIs), three of which had not been evaluated against FIV in feline cells before. (uni-muenchen.de)
  • In a Cox model, less protease inhibitors and nucleoside reverse transcriptase inhibitors (NRTIs) previously used, higher CD4 nadir, lower viral load at baseline, a previous AIDS diagnosis and less NRTIs in the regimen were associated with lower risk of virological failure. (ovid.com)
  • X rays diffraction and NMR studies of free or inhibitor-bound RT have led to the recognition of RT 3D structure, and allowed a thorough understanding of the mode of action of classical competitive nucleoside RT inhibitors (NRTIs) and of the binding of allosteric, non NRTIs (NNRTIs) inhibitors. (eurekaselect.com)
  • By contrast with NRTIs, they seem to block initiation steps of reverse transcription. (eurekaselect.com)
  • BACKGROUND: Nucleoside reverse-transcriptase inhibitors (NRTIs), which are used to treat human immunodeficiency virus (HIV) infection, can cause mitochondrial dysfunction and have been associated with lipoatrophy. (garvan.org.au)
  • METHODS: We studied patients from the Swiss HIV Cohort Study who failed cART with nucleoside reverse transcriptase inhibitors (NRTIs) and either a ritonavir-boosted PI (PI/r) or a non-nucleoside reverse transcriptase inhibitor (NNRTI). (uzh.ch)
  • Two of the main classes of HIV drugs are nucleoside reverse transcriptase inhibitors (NRTIs) and protease inhibitors. (pubmedcentralcanada.ca)
  • However, two rare, novel mutations, Q145M/L, have been reported to cause high-level resistance to multiple NRTIs and NNRTIs, even in the absence of other known RT inhibitor resistance mutations. (asm.org)
  • Nucleoside reverse transcriptase inhibitors (NRTIs) are mainstay therapeutics for HIV that block retrovirus replication. (cdc.gov)
  • We found that NRTIs inhibit P2X7-mediated NLRP3 inflammasome activation independent of reverse transcriptase inhibition. (cdc.gov)
  • Nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs) are a class of medication known as antivirals. (verywellhealth.com)
  • For newly diagnosed HIV infections, NRTIs are used in combination with an integrase inhibitor. (verywellhealth.com)
  • The panel concluded that other effective regimens may include nonnucleoside reverse transcriptase inhibitors or boosted protease inhibitors with two NRTIs. (thefreedictionary.com)
  • The first-line regimen HAART mainly targets reverse transcriptase (RT) through the employment of two nucleoside RT inhibitors (NRTIs) and a nonnucleoside RT inhibitor (NNRTI). (sun.ac.za)
  • As 'n eerste behandeling, teiken HAART meestal trutranskriptase (RT) deur die inspanning van twee nukleosied trutranskriptase inhibeerders (NRTIs) en 'n nie-nukleosied trutranskriptase inhibeerder (NNRTI). (sun.ac.za)
  • Of these three enzymatic drug targets, only the RTIs have two classifications based on their modus operandi as nucleoside RT inhibitors (NRTIs) and non-nucleoside RT inhibitors (NNRTIs). (bioscirep.org)
  • The NNRTIs functions non-competitively, binding to an allosteric site to cause structural changes to the RT polymerase active site, whereas the NRTIs directly compete in the active site with nucleotides during the incorporation to terminate the reverse-transcription process [ 3 ]. (bioscirep.org)
  • Nucleoside reverse transcriptase inhibitors (NRTIs) block reverse transcriptase (an HIV enzyme). (hiv.gov)
  • The Food and Drug Administration (FDA)-approved nucleos(t)ide reverse transcriptase inhibitors (NRTIs) include zidovudine (ZDV), stavudine (d4T), didanosine (ddI), abacavir (ABC), tenofovir disoproxil fumarate (TDF), tenofovir alafenamide (TAF), lamivudine (3TC), and emtricitabine (FTC). (hiv.gov)
  • A handful of experimental therapies in the three approved classes -- protease inhibitors (PIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), and nucleoside reverse transcriptase inhibitors (NRTIs) -- may provide benefit to people who are in need of third-line therapy, that is, those whose dominant HIV isolates (strains) have become resistant to many or all of the currently available drugs. (thebody.com)
  • Several classes of anti-HIV drugs interfere with this stage of HIV's life cycle: nucleoside reverse transcriptase inhibitors and nucleotide reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs). (aidsmap.com)
  • Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are antiretroviral drugs used in the treatment of human immunodeficiency virus (HIV). (wikipedia.org)
  • NNRTIs inhibit reverse transcriptase (RT), an enzyme that controls the replication of the genetic material of HIV. (wikipedia.org)
  • The development of NNRTIs improved quickly into the 1990s and they soon became the third class of antiretroviral drugs, following the protease inhibitors. (wikipedia.org)
  • NNRTIs block reverse transcriptase by binding directly to the enzyme. (wikipedia.org)
  • NNRTIs are therefore classified as non-competitive inhibitors of reverse transcriptase. (wikipedia.org)
  • Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are the third class of antiretroviral drugs that were developed. (bionity.com)
  • Non-nucleoside reverse transcriptase inhibitors (NNRTIs) interfere with reverse transcriptase by binding directly to the enzyme. (aidsmap.com)
  • Non-nucleoside reverse transcriptase inhibitors (NNRTIs), their discovery, development, and use in the treatment of HIV-1 infection: a review of th. (nih.gov)
  • It describes the characteristics of the NNRTIs, their mechanisms of action, HIV-1 resistance to the inhibitors, and the drugs that have been approved for the treatment of HIV-1 infection, or are currently in clinical development. (nih.gov)
  • In this scenario, our recently reported triazole non-nucleoside reverse-transcriptase inhibitors (NNRTIs) [ 6 ] ( Figure 1 ) have emerged as very suitable pharmacophore structures. (mdpi.com)
  • SAN DIEGO, April 7, 2008, 2008 /PRNewswire-FirstCall/ -- Ardea Biosciences, Inc. today announced that data will be presented on its second generation non-nucleoside reverse transcriptase inhibitors (NNRTIs), at the 21st International Conference on Antiviral Research (ICAR). (drugs.com)
  • This review gives an overview of the disease and addresses the drugs currently used for treatment, with specific emphasis on new developments within the class of allosteric non-nucleoside reverse transcriptase inhibitors (NNRTIs). (rsc.org)
  • Thirty percent of women who receive NVP, either alone or as part of a non-suppressive regimen, will develop high-level drug resistance to antiretroviral therapy (ART) with non-nucleoside reverse transcriptase inhibitors (NNRTIs). (ucsf.edu)
  • Current NNRTIs represent, in terms of chemical structures, a heterogeneous class of inhibitors currently undergoing extensive development. (eurekaselect.com)
  • The M230L mutation in HIV-1 reverse transcriptase (RT) is associated with resistance to first-generation nonnucleoside reverse transcriptase inhibitors (NNRTIs). (pubmedcentralcanada.ca)
  • Nonnucleoside reverse transcriptase inhibitors (NNRTIs), which include first-generation drugs such as nevirapine (NVP) and efavirenz (EFV), are important components of HAART, as is a newer agent, etravirine (ETR), which retains activity against HIV type 1 variants containing common drug resistance mutations, such as K103N, associated with the diminished activity of NVP and EFV. (pubmedcentralcanada.ca)
  • Nonnucleoside reverse transcriptase inhibitors (NNRTIs) are a potent component in salvage therapy. (thefreedictionary.com)
  • In addition to the protease inhibitors and the nonnucleoside reverse transcriptase inhibitors (or NNRTIs), new and more powerful second-generation nucleoside analogues (such as lamivudine-3TC) are now also available. (thefreedictionary.com)
  • They conducted a retrospective chart review from 41 PI experienced patients, which revealed that 73% were also experienced with nonnucleoside reverse transcriptase inhibitors (NNRTIs). (thefreedictionary.com)
  • NNRTIs teiken 'n allosteriese leemte wat ongeveer 10 Å weg van die katalitiese posisie is en veroorsaak dan 'n konformasie verandering in die ensiem tydens die bindingsproses, wat dan lei tot die inhibisie van die virus se replikasie. (sun.ac.za)
  • HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs) are part of the combination therapy currently used to treat HIV infection. (rcsb.org)
  • Dapivirine (TMC120) is a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of HIV-1 isolates from different classes, inclucing a wide range of NNRTI-resistant isolates. (selleckchem.com)
  • Department of Health and Human Services (DHHS) list the combination of efavirenz, emtricitabine and tenofovir disoproxil fumarate as one of the preferred non-nucleoside reverse transcriptase inhibitor (NNRTI)-based treatment regimens for use in appropriate patients who have never taken anti-HIV medicines before. (thefreedictionary.com)
  • Department of Health and Human Services (DHHS) list emtricitabine and tenofovir disoproxil fumarate as preferred agents for use as part of a non-nucleoside reverse transcriptase inhibitor (NNRTI)-based regimen in appropriate patients who have never taken anti-HIV medicines before. (thefreedictionary.com)
  • Nevirapine is a non-nucleoside reverse transcriptase inhibitor (NNRTI), manufactured by Boehringer Ingelheim Pharmaceuticals, Inc. (thefreedictionary.com)
  • Delavirdine is a non-nucleoside reverse transcriptase inhibitor (NNRTI), manufactured by Pharmacia & Upjohn. (thefreedictionary.com)
  • Nevirapine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used to treat HIV-1 infection and AIDS. (selleckchem.com)
  • More recently, clinical trials examining these dual-NRTI combinations with a protease inhibitor (PI), nonnucleoside reverse transcriptase inhibitor (NNRTI), or 3rd NRTI documented sustained reductions in viral load and a normalization of CD4 cell counts. (natap.org)
  • An NNRTI of HIV-1, delavirdine directly binds to reverse transcriptase and inhibits RNA- and DNA-dependent DNA polymerase. (medscape.com)
  • Etravirine is an NNRTI of HIV-1 that binds directly to reverse transcriptase, causing catalytic site disruption. (medscape.com)
  • Nevirapine is an NNRTI that limits virus replication by a mechanism different from the nucleosidase inhibitors such as zidovudine and lamivudine. (medscape.com)
  • Rilpivirine is a NNRTI that inhibits HIV-1 replication by noncompetitive inhibition of HIV-1 reverse transcriptase. (medscape.com)
  • A non-nucleoside reverse transcriptase inhibitor (NNRTI) used in the treatment of HIV-1 infections in combination with other antiretroviral agents. (drugbank.ca)
  • A non-nucleoside reverse transcriptase inhibitor (NNRTI) used in combination with other antiretrovirals to specifically treat human immunodeficiency virus type 1 (HIV-1). (drugbank.ca)
  • Our most advanced drug candidate is RDEA806, a non-nucleoside reverse transcriptase inhibitor (NNRTI), which is in a Phase 2a study for the treatment of HIV. (drugs.com)
  • We recently demonstrated that a formulation of the nonnucleoside reverse transcriptase inhibitor (NNRTI) MIV-150 in carrageenan reduced vaginal infection of macaques with simian immunodeficiency virus SIVmac239 with HIV-1_HXB2 reverse transcriptase (SHIV-RT). (popcouncil.org)
  • To assess the factors associated with virologic response to non-nucleoside reverse transcriptase inhibitor (NNRTI)-containing regimens in a large clinic cohort. (ovid.com)
  • OBJECTIVE: To compare the characteristics of patients prescribed non-nucleoside reverse transcriptase inhibitors (NNRTI) and protease inhibitors (PI), and evaluate treatment outcomes in a setting in which nevirapine has been preferentially recommended since 1998. (ubc.ca)
  • The drug cocktail can comprise all three classes of HIV inhibitors, including nucleoside reverse transcriptase inhibitors (NRTI), non-nucleoside reverse transcriptase inhibitors (NNRTI) and protease inhibitors (PI). (eurekaselect.com)
  • Although the reverse transcriptase (RT) mutations responsible for most nucleoside RT inhibitor (NRTI)- and nonnucleoside RT inhibitor (NNRTI)-resistant viruses are known, there have been recent reports that several less widely recognized RT mutations may also decrease RT inhibitor susceptibility, usually in combination with one or more of the known drug resistance mutations (reviewed in reference 10 ). (asm.org)
  • To develop a high-throughput, real-time reverse transcriptase (RT) polymerase chain reaction (PCR) assay to quantify non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant variants K103N (AAT or AAC alleles) at frequencies as low as 0.1%, and to apply this to monitor these variants before, during, and after NNRTI therapy. (actgnetwork.org)
  • On the other hand, the NNRTI allosteric inhibitors that distantly influence the RT polymerase active site, is open to a wider scope of ligand structures. (bioscirep.org)
  • Based on analogy with known HIV-1 NNRTI inhibitors and modeling studies utilizing the X-ray crystal structure of inhibitors bound in the HIV-1 RT, a series of substituted 2-quinolones was synthesized and evaluated as HIV-1 inhibitors. (rcsb.org)
  • Abacavir is a nucleoside reverse transcriptase inhibitor (NRTI). (thefreedictionary.com)
  • Both Truvada and Combivir are widely used fixed-dose combination medicines from the nucleoside reverse transcriptase inhibitor (NRTI) class of antiretrovirals. (thefreedictionary.com)
  • Several dual nucleoside reverse transcriptase inhibitor (NRTI) combinations provide efficacy when combined with a 3rd agent. (natap.org)
  • However, there are a number of issues with current NRTI and nucleotide reverse transcriptase inhibitor (NtRTI) combinations that often lead to treatment failure and limited treatment options. (natap.org)
  • Early nucleoside reverse transcriptase inhibitor (NRTI) backbone combinations improved upon the results seen with nucleoside monotherapy and included lamivudine (3TC) + zidovudine (ZDV), ZDV + didanosine (ddI), 3TC + stavudine (d4T), and ddI + d4T. (natap.org)
  • Gilead study 903 showed that the nucleotide reverse transcriptase inhibitor (NtRTI) tenofovir DF (TDF), when combined with 3TC and EFV, showed similar efficacy compared with d4T + 3TC + EFV but had fewer NRTI-associated toxicities and led to more favorable lipid profiles. (natap.org)
  • The background dual nucleoside reverse transcriptase inhibitor (NRTI) antiretroviral therapy (ART) for all arms will be either abacavir/lamivudine (ABC/3TC) or tenofovir/emtricitabine (TDF/FTC) as selected by the Investigator. (clinicaltrials.gov)
  • The primary purpose of this research study is to evaluate the safety and tolerability of raltegravir 400 mg taken twice a day compared to an NRTI (nucleotide reverse transcriptase inhibito. (bioportfolio.com)
  • The aim of this study was to investigate whether specific nucleoside reverse transcriptase inhibitor (NRTI) backbones are associated with risk of adverse pregnancy outcomes among pregnant women starti. (bioportfolio.com)
  • We conducted a viral dynamics substudy of A5142, a trial comparing lopinavir (LPV)/ritonavir with efavirenz (LPV/EFV) versus LPV and two nucleoside reverse transcriptase inhibitor (NRTI) (LPV) versus EFV and two NRTI (EFV) in antiretroviral (ARV)-naive individuals. (actgnetwork.org)
  • Case reports indicate St. John's wort also lowers blood levels of the non-nucleoside reverse transcriptase inhibitor nevirapine. (portsmouthhospital.com)
  • Nevirapine (NVP) itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki = 270 mM). [1] Nevirapine is a non-nucleoside RT inhibitor with a well-characterized inhibitory activity on RT enzymes of retroviral origin. (selleckchem.com)
  • Nevirapine is also an effective inhibitor of the endogenous RT in murine and human cell lines. (selleckchem.com)
  • [2] Nevirapine, a dipyridodiazepinone, is a highly specific inhibitor of HIV-1 reverse transcriptase (RT) which exhibits an IC50 = 84 nM in enzyme assays and IC50 = 40nM against HIV-1 replication in cell culture. (selleckchem.com)
  • The results of molecular modeling and docking confirmed that all compounds assumed a butterfly-like conformation and showed H-bond, 'π-π' and 'π-+' and hydrophobic interactions within flexible non-nucleoside inhibitor binding pocket of HIV-1 reverse transcriptase, similar to known non-nucleoside reverse transcriptase inhibitors, such as nevirapine. (sigmaaldrich.com)
  • A 3.5 angstrom resolution electron density map of the HIV-1 reverse transcriptase heterodimer complexed with nevirapine, a drug with potential for treatment of AIDS, reveals an asymmetric dimer. (sciencemag.org)
  • Efavirenz and nevirapine are widely used non-nucleoside reverse transcriptase inhibitors for the treatment of HIV infection. (biomedcentral.com)
  • Development is also arrested when the embryo endogenous RT activity is pharmacologically inhibited by nevirapine, an RT inhibitor currently employed in AIDS treatment. (mdpi.com)
  • The reverse transcriptase inhibitors lamivudine and zidovudine can cause damage to the mitochondria, the energy-producing subunits of cells. (portsmouthhospital.com)
  • Although the idea of combining three nucleoside reverse transcriptase inhibitors seemed appealing as a way to spare patients some of the toxicities of nonnucleoside reverse transcriptase inhibitors or protease inhibitors, once-daily triple-nucleoside combinations that lacked zidovudine (AZT) often failed because of gene mutations, which were infrequently seen in the past when nearly every regimen contained AZT, investigators reported at the meeting. (thefreedictionary.com)
  • Zidovudine, as the triphosphate, was the first anti-HIV drug to be introduced and has a high affinity for reverse transcriptase. (clicktocurecancer.info)
  • Rarely, a syndrome of hepatic necrosis with lactic acidosis may occur with zidovudine (and with other reverse transcriptase inhibitors). (clicktocurecancer.info)
  • Despite significant pharmacological advances, the backbone of the most highly active antiretroviral therapy regimens for controlling HIV/AIDS is still a combination of reverse transcriptase inhibitors (RTIs) first discovered in the late 1980s. (springer.com)
  • To examine the impact of transmitted drug resistance (TDR) on response to first-line regimens with integrase strand transfer inhibitors (INSTIs) or boosted protease inhibitors (bPIs). (bioportfolio.com)
  • Integrase inhibitor-based regimens result in more rapid virologic suppression rates among treatment-naïve human immunodeficiency virus-infected patients compared to non-nucleoside and protease inhibitor-based regimens in a real-world clinical setting: A retrospective cohort study. (bioportfolio.com)
  • The integrase strand transfer inhibitor (INSTI) class of antiretroviral therapy (ART) may result in faster time to virologic suppression compared with regimens that contain protease inhibitors (PIs) o. (bioportfolio.com)
  • In Reverse Transcriptase Inhibitors in HIV/AIDS Therapy, leading experts in AIDS/HIV drug discovery and development review all aspects of RTIs (nucleosides, nucleotides, and non-nucleosides), including drug discovery, pharmacology, development of drug resistance, toxicity, and prevention of mother-to-child transmission of HIV/AIDS. (springer.com)
  • Reverse-transcriptase inhibitors (RTIs) are a class of antiretroviral drugs used to treat HIV infection or AIDS, and in some cases hepatitis B. RTIs inhibit activity of reverse transcriptase, a viral DNA polymerase that is required for replication of HIV and other retroviruses. (wikipedia.org)
  • RTIs block reverse transcriptase's enzymatic function and prevent completion of synthesis of the double-stranded viral DNA, thus preventing HIV from multiplying. (wikipedia.org)
  • Reverse transcriptase inhibitors (RTIs) are a class of antiretroviral drug used to treat HIV infection. (bionity.com)
  • RTIs inhibit activity of reverse transcriptase , a viral DNA polymerase enzyme that HIV needs to reproduce. (bionity.com)
  • The first aim of this study was to investigate whether APHS can act synergically with the clinically available reverse transcriptase and protease inhibitors (RTIs and PIs, respectively) in vitro. (rug.nl)
  • As part of a program to develop an effective prevention strategy, we performed an ex-vivo preclinical evaluation to determine the efficacy of multiple double combinations of maraviroc (MVC) and reverse transcriptase inhibitors (RTIs). (www.gov.uk)
  • Design: The entry inhibitor, MVC, a nucleotide RTI, tenofovir and two non-nucleoside RTIs, UC781 and TMC120 (dapivirine, DPV), were used in double, combinations against a panel of CCR5-using clade B and clade C HIV-1 isolates and against MVC-escape variants. (www.gov.uk)
  • Currently, the HAART cocktail consists of reverse transcriptase (RT) inhibitors (RTIs), protease inhibitors, and integrase inhibitors. (bioscirep.org)
  • A magisterial survey of all aspects of the reverse transcriptase inhibitors (RTIs) used to treat HIV/AIDS, including drug discovery, pharmacology, development of drug resistance, toxicity, and prevention of mother-to-child transmission of HIV/AIDS. (readrate.com)
  • The authors point to evidence that antiretrovirals in the nucleoside/nucleotide reverse transcriptase inhibitor class can inhibit the ability of SARS-CoV-2 (the virus that causes COVID-19 disease) to bind with human cells. (aidsmap.com)
  • Conclusion: This study demonstrates that combinations based on antiretroviral drugs inhibiting HIV transmission at viral entry and reverse transcription have potential as prevention strategies against colorectal transmission of HIV-1 including MVC-resistant isolates. (www.gov.uk)
  • Objectives: An increasing number of HIV-infected patients are combating HIV infection through the use of antiretroviral drugs, including reverse transcriptase inhibitors. (elsevier.com)
  • We tested the safety and antiviral efficacy of a novel combination consisting of efavirenz, nelfinavir, and one or more nucleoside reverse-transcriptase inhibitors in 57 children previously treated with only nucleoside reverse-transcriptase inhibitors. (ebscohost.com)
  • Conclusions: In HIV-1â€"infected children who were previously treated with nucleoside reverse-transcriptase inhibitors, the combination of efavirenz, nelfinavir, and nucleoside reverse-transcriptase inhibitors was generally well tolerated and had a potent and sustained antiviral effect. (ebscohost.com)
  • Thus though the child is now on a protease inhibitor {LPVr}, whether Abacavir and Didanosine will work or not is not known. (pediatriconcall.com)
  • Abacavir (t'/2 2 h) may be the most potent reverse transcriptase inhibitor. (clicktocurecancer.info)
  • Results suggesting associations with specific nucleoside reverse transcriptase inhibitor combinations need further investigations. (nih.gov)
  • In phase 1 trials, the HIV-1 integrase strand transfer inhibitor cabotegravir (GSK1265744) was well tolerated, both alone, and in combination with the non-nucleoside reverse transcriptase inhibitor rilpivirine. (natap.org)
  • On the other hand, rilpivirine (RPV)-resistant mutations showed the highest cross-resistance to the other non-nucleoside RT inhibitors. (bioscirep.org)
  • Pacific Time Title: RDEA119, a Potent and Highly Specific MEK Inhibitor is Efficacious in Mouse Tumor Xenograft Studies Location: Poster Session 32 (Poster #4878), Exhibit Hall B-F Date/Time: Tuesday, April 15, 2008 at 1:00 p.m. (drugs.com)
  • In view of the results obtained, it can be said that the chemical skeletons of N, N'-bis-(pyridin-2-yl)-succinamide (14 and 15) and 1, 4-bis-benzoimidazol-1-yl-butane-1, 4-dione (16 and 17) may be used for developing potent inhibitors of HIV-1 replication, with suitable structure/pharmacophore modifications. (sigmaaldrich.com)
  • The multidrug, single- or multiple-target therapies have revived the development of new and more potent RT inhibitors. (aspetjournals.org)
  • It is a potent inhibitor of various mutant viral variants that have emerged. (aspetjournals.org)
  • Women with persistently high viral loads could be switched to a ritonavir-based protease inhibitor at the clinician's discretion. (ucsf.edu)
  • Drugs like saquinavir , ritonavir , nelfinavir, indinavir and amprenavir are some of the protease inhibitors. (medindia.net)
  • Its European licence specifies that it must be used in a protease inhibitor (PI)-boosted HAART regimen. (aidsmap.com)
  • Evidence from the only national random sample of HIV patients (the HIV Cost and Services Utilization Study--HCSUS) also found that women were less likely to receive therapies involving protease inhibitors or nonnucleoside reverse transcriptase inhibitors (therapy involving these drugs is often referred to as highly active antiretroviral therapy or HAART) immediately after their diffusion (Shapiro et al. (thefreedictionary.com)
  • HAART generally includes nucleoside reverse transcriptase inhibitors and protease inhibitors. (biomedcentral.com)
  • Over the past two decades, novel drugs for HIV-1 antiretroviral therapy have improved long-term viral suppression.1 The discovery of integrase strand transfer inhibitors (INIs) has provided important treatment options for patients with HIV/AIDS. (natap.org)
  • The survey, which looked at specimens from 3,130 newly diagnosed, drug-naive individuals, found that 4% of infections had mutations conferring resistance to nucleoside reverse transcriptase inhibitors, 7% to nonnucleoside reverse transcriptase inhibitors , and 2% to protease inhibitors. (thefreedictionary.com)
  • Preclinical in vitro data for elvucitabine showed that elvucitabine has a plasma protein binding of less than 10%, is metabolized intracellularly into monophosphate, diphosphate, and triphosphate analytes (with elvucitabine triphosphate having a half-life of at least 20 h), has no other significant metabolites (i.e., was not metabolized by CYP enzymes), and is not an inducer or an inhibitor of CYP enzymes. (pubmedcentralcanada.ca)
  • Impact of transmitted HIV-1 drug resistance on the efficacy of first-line antiretroviral therapy with two nucleos(t)ide reverse transcriptase inhibitors plus an integrase inhibitor or a protease inhibitor. (bioportfolio.com)
  • Integrase inhibitor The integrase inhibitors raltegravir, elvitegravir and dolutegravir prevent the replication of the HIV virus. (medindia.net)
  • Comprehensive and up-to-date, Reverse Transcriptase Inhibitors in HIIV/AIDS Therapy offers a magisterial survey of the discovery, clinical development, current use, and future possibilities of all drugs that treat HIV/AIDS by inhibiting the viral reverse transcriptase. (springer.com)
  • It then competes with cellular triphosphates, which are substrates for proviral DNA by viral reverse transcriptase. (drugs.com)
  • Replication of human immunodeficiency virus 1 (HIV-1) uses a viral reverse transcriptase (RT) to convert its positive-strand RNA into double stranded DNA, which is then integrated into host genome. (eurekaselect.com)
  • When HIV enters a healthy CD4 cell-part of the body's immune system-the virus tries to copy its RNA into DNA via a process called reverse transcription, which requires an enzyme reverse transcriptase. (verywellhealth.com)
  • this crucial conversion, the reverse of the normal cellular transcription of nucleic acids, is accomplished by the enzyme reverse transcriptase. (clicktocurecancer.info)
  • Synthesis and antiviral evaluation of carbocyclic nucleoside analogs of nucleoside reverse transcriptase translocation inhibitor MK-8591 (4'-ethynyl-2-fluoro-2'-deoxyadenosine). (bioportfolio.com)
  • MK-8591 (4'-ethynyl-2-fluoro-2'-deoxyadenosine) is a novel nucleoside analog that displays a differentiated mechanism of action as a nucleoside reverse transcriptase translocation inhibitor (NRTTI) co. (bioportfolio.com)
  • To study the mechanisms of these mutations in conferring drug resistance, we computationally analyzed 14 reverse transcriptase (RT) structures of HIV-1 on the following parameters: drug-binding pocket volume, allosteric effects caused by the mutations, and structural thermal stability. (bioscirep.org)
  • Through computational analyses, we found such a novel druggable pocket on the HIV-1 RT structure that is comparable with the original allosteric drug site, opening the possibility to the design of new inhibitors. (bioscirep.org)
  • when used in this way they are referred to as polymerase inhibitors. (wikipedia.org)
  • Does Tenofovir-containing First-line Antiretroviral Therapy Mitigate the Impact of Pretreatment Non-nucleoside Reverse Transcriptase Inhibitor Drug Resistance? (ox.ac.uk)
  • Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. (rcsb.org)
  • These are categorized by drug class: nucleoside analogs, nonnucleoside reverse transcriptase inhibitors , and protease inhibitors. (thefreedictionary.com)
  • We report that Q145M and other Q145 mutations do not emerge with RT inhibitors nor decrease RT inhibitor susceptibility. (asm.org)
  • Specifically, we determined whether mutations at RT position 145 were selected by RT inhibitors, contributed to decreased RT inhibitor susceptibility, or interfered with a virological response to RT inhibitors. (asm.org)
  • Columns 6 through 8 show that in a large database of HIV-1 RT sequences from a commercial reference laboratory, Q145 mutations were as likely to occur in viruses without RT mutations as they were to occur in viruses with RT inhibitor resistance mutations. (asm.org)
  • This lack of association with RT inhibitor therapy and RT inhibitor resistance mutations demonstrates that Q145 mutations are not selected by RT inhibitor therapy. (asm.org)
  • Maraviroc is an approved CCR5 antagonist, also called entry inhibitor. (medindia.net)
  • A non-nucleoside reverse transcriptase inhibitor used as part of a management regimen for HIV-1 virus infection. (drugbank.ca)
  • Molecular modeling, synthesis and biological evaluation of N-heteroaryl compounds as reverse transcriptase inhibitors against HIV-1. (sigmaaldrich.com)
  • Greatly improved processivity of SuperScript IV RT allows cDNA synthesis even in the presence of common inhibitors such as guanidinium and salts. (thermofisher.com)
  • Some oncogenic RNA virus under the action of an enzyme produced by itself, is able of RNA as a template,according the RNA nucleotide sequence to the synthesis of DNA, this enzyme is called Reverse Transcriptase. (conbottpharm.com)
  • The authors synthesize our current understanding of the role of reverse transcriptase in the viral life cycle, describe the discovery and development of eight nucleoside and nucleotide analogs that represent milestones in treatment history, and thoroughly discuss the question of toxicity and resistance to this class of drugs. (springer.com)
  • Children in this study will receive a combination of at least three drugs that include at least one protease inhibitor and one reverse transcriptase inhibitor. (clinicaltrials.gov)
  • The children will either continue to receive the anti-HIV drugs they have been taking, or their medicines will be changed to a different combination of protease inhibitor and reverse transcriptase inhibitor. (clinicaltrials.gov)
  • Determine the specificity of the anti-retroviral drugs to inhibit cellular reverse transcriptase and reduce human neurodegeneration. (ca.gov)
  • Fusion inhibitors are drugs that prevent HIV from entering the cells. (medicalnewstoday.com)
  • These drugs prevent HIV replication by blocking the reverse transcriptase enzyme that converts RNA to DNA. (medindia.net)
  • Protease inhibitors are drugs which inhibit the protease enzyme of the HIV virus that is necessary for viral replication and infectivity. (medindia.net)
  • Q145M should not, therefore, be considered an RT inhibitor resistance mutation. (asm.org)
  • Rather, in the presence of saturating concentrations of the inhibitors, the nucleoside triphosphate bound tightly (Kd, 100 nM), but nonproductively. (nih.gov)
  • Providing inhibitory concentrations of HIV-1 reverse transcriptase inhibitors to impede the replication of the virus in the female genital tissue offers a mechanism for prophylaxis of HIV-1. (www.gov.uk)
  • Reverse Transcriptase can inhibit activity of this enzyme , Transcriptase Inhibitors can be divided nucleoside Reverse Transcriptase Inhibitors NRTLs and non-nucleoside Reverse Transcriptase Inhibitors NNRTLs according the main chemical structure currently. (conbottpharm.com)
  • Nucleoside reverse transcriptase inhibitors, mitochondrial DNA and AIDS therapy. (nih.gov)
  • The data suggest that an inhibitor combining the functionalities of a nonnucleoside inhibitor and a nucleotide analog could bind very tightly and specifically to reverse transcriptase and could be effective in the treatment of AIDS. (nih.gov)
  • The children who will be evaluated and followed in this study are those who have previously been studied on other protease inhibitor-containing anti-HIV protocols within the HIV and AIDS Malignancy Branch. (clinicaltrials.gov)
  • Which medications in the drug class Antiretroviral agent, non-nucleoside reverse-transcriptase inhibitor are used in the treatment of HIV Infection and AIDS? (medscape.com)
  • Enfuvirtide is one fusion inhibitor, and it has the brand name Fuzeon. (medicalnewstoday.com)
  • Fusion inhibitor A fusion inhibitor prevents the entry of the HIV virus into the CD4 cells. (medindia.net)
  • Enfuvirtide is an approved fusion inhibitor. (medindia.net)
  • Reverse transcription is a complex event involving p66 and p51 RT subunits but also several viral proteins including Nef, Tat, Vif, IN, NCp7 and p55gag. (eurekaselect.com)
  • HIV uses reverse transcriptase to convert its RNA into DNA (reverse transcription). (hiv.gov)
  • Blocking reverse transcriptase and reverse transcription prevents HIV from replicating. (hiv.gov)
  • Inhibitors can significantly impair the efficiency of reverse transcription reactions. (thermofisher.com)
  • Sensitivity and dynamic range in reverse transcription are important factors for accurate quantitation in RT-qPCR. (thermofisher.com)
  • Consistent with this, recent findings indicate that a reverse transcription wave is triggered in the zygote a few hours after fertilization and is propagated at least through the first two rounds of cell division. (mdpi.com)
  • On the whole these findings suggest that reverse transcription is strictly required in early embryos as a key component of a novel RT-dependent mechanism that regulated the proper unfolding of the developmental program. (mdpi.com)
  • Entecavir hydrate CAS NO 209216 23 9 is a nucleoside analog more specifically a guanine analogue that inhibits reverse transcription DNA replication and transcription in the viral replication process Thera Category Adult chronic hepatitis B Cas No. (conbottpharm.com)
  • Rinvoq (upadacitinib) is a Janus kinase (JAK) inhibitor for the treatment of. (drugs.com)
  • Inrebic (fedratinib) is a highly selective JAK2 inhibitor for the treatment of. (drugs.com)
  • In the United States and the European Union, Truvada is indicated in combination with other antiretroviral agents (such as non-nucleoside reverse transcriptase inhibitors or protease inhibitors) for the treatment of HIV-1 infection in adults. (thefreedictionary.com)
  • This study will continue to follow children who participated in an earlier National Cancer Institute trial of HIV treatment with a protease inhibitor. (clinicaltrials.gov)
  • Our lead mitogen-activated ERK kinase (MEK) inhibitor, RDEA119, is in a Phase 1 study in advanced cancer patients and is being investigated for the treatment of inflammatory diseases. (drugs.com)
  • RDEA436, our second generation MEK inhibitor for the treatment of cancer and inflammatory diseases, has been evaluated in a human micro-dose pharmacokinetic study and has been selected as a development candidate. (drugs.com)
  • Long-term studies of tolerance to perinatal exposure to antiretroviral nucleoside reverse transcriptase inhibitors are required, in view of the potential genotoxicity of some of these molecules. (nih.gov)