NRTIsNRTINNRTITenofovir disoproxLamivudineProtease inhibitorNNRTIsIntegrase strand transfer inhibitorsStavudineRegimensNucleotide analogCarbocyclic nucleosideAntiviral ActivityRegimenAntiretroviralsStructurallyAIDSInhibitionSynthesisEnzymeMonotherapySubstrateGenomeTriphosphateHepatitisTranscriptionNucleotidesViral infectionsEfficacyCellularToxicityCombinationAffinityDerivativesPatientsClassDrugsZiagenChronicSyntheticCommonlyTreatCasesTypeVirusesMethodsSafety
NRTIs13
- Most experts currently believe that HIV type 1 (HIV-1) protease inhibitors (PIs) and nucleoside reverse transcriptase inhibitors (NRTIs), especially stavudine and zidovudine, are implicated. (medscape.com)
- Both are antiviral medicines also known as antiretrovirals, called nucleoside analogue reverse transcriptase inhibitors (NRTIs). (who.int)
- Lamivudine is in a class of medications called nucleoside analogue reverse transcriptase inhibitors (NRTIs) and dolutegravir is in a class of medications called integrase strand transfer inhibitors (INSTIs). (medlineplus.gov)
- Our model correctly predicts for HIV-1 that resistance against nucleoside analog reverse transcriptase inhibitors (NRTIs) can be conferred by decreasing their incorporation rate, increasing their excision rate, or decreasing their affinity for the polymerase enzyme. (plos.org)
- Nucleoside reverse transcriptase inhibitors (NRTIs) block reverse transcriptase (an HIV enzyme). (hiv.gov)
- 50 copies per millilitre (c/mL), a standard measure of HIV control, at week 48 when compared to a three-drug regimen of dolutegravir and two nucleoside reverse transcriptase inhibitors (NRTIs), tenofovir disoproxil fumarate/emtricitabine (TDF/FTC), in treatment-naïve, HIV-1 infected adults. (gsk.com)
- A section of the drug known as Zidovudine, also known as AZT which is a part of Nucleoside analogue reverse-transcriptase inhibitors NRTIs were the first of their kind to serve as a treatment for HIV. (healthjockey.com)
- NNRTI na ve patients with prior nucleoside analogue reverse transcriptase inhibitor (NRTI) exposure, who have isolates with resistance mutations and phenotypic resistance to NRTIs, appear more likely to have hypersusceptibility to the NNRTI class of drugs. (antimicrobe.org)
- The aim was to study the mitochondrial toxicities in terms of peripheral neuropathy (PN), lipodystrophy (LD), hepatic steatosis, lactic academia (LA), and pancreatitis developing in AIDS cases on nucleoside analog reverse transcriptase inhibitors (NRTIs) based ART regimens. (ijstd.org)
- Both the medicines belong to the group of medications known as antiretrovirals, called nucleoside analogue reverse transcriptase inhibitors (NRTIs). (alldaychemist.com)
- Delstrigo combines doravirine, a new non-nucleoside reverse transcriptase inhibitor (NNRTI), with lamivudine and tenofovir disoproxil fumarate, 2 nucleoside analogue reverse transcriptase inhibitors (NRTIs). (infectiousdiseaseadvisor.com)
- Because TS inhibitors modulate intracellular concentrations of endogenous 2'-deoxynucleotides, we hypothesized that TS inhibitors could impact the anti-HIV activity of nucleoside analogue reverse transcriptase inhibitors (NRTIs). (bvsalud.org)
- METHODS: We evaluated gemcitabine and pemetrexed, two approved TS inhibitors, on the anti-HIV activities of NRTIs in infectivity assays using peripheral blood mononuclear cells (PBMCs) and in humanized mice. (bvsalud.org)
NRTI5
- A nucleoside analogue reverse transcriptase inhibitor (NRTI) with antiretroviral activity against HIV, it is used (particularly as the sulfate) with other antiretrovirals in combination therapy of HIV infection. (chemspider.com)
- Through mathematical modeling, we assess the mechanisms by which HIV-1 can develop resistance against nucleoside analog reverse transcriptase inhibitors (NRTI). (plos.org)
- This study evaluated the safety and efficacy of switching HIV-infected patients with stable viral suppression on nonnucleoside reverse transcriptase inhibitor/nucleoside reverse transcriptase inhibitor (NNRTI/NRTI) therapy to lopinavir/ritonavir (LPV/r) monotherapy. (researchgate.net)
- It is a nucleoside reverse transcriptase inhibitor (NRTI), guanosine analogue used for HIV treatment . (shimclinic.com)
- Abacavir (ABC) is a powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS. (newedgeoverseas.com)
NNRTI2
- FTC 120 mg/TAF 15 mg, in combination with an integrase strand transfer inhibitor (INSTI) or a non-nucleoside reverse transcriptase inhibitor (NNRTI). (hiv.gov)
- This study compared the accuracy of molecular descriptors from two cheminformatics Mordred and PaDEL, software libraries, in characterizing the chemo-structural composition of 53 compounds from the non-nucleoside reverse transcriptase inhibitors (NNRTI) class. (emerginginvestigators.org)
Tenofovir disoprox2
- Results Nephrotoxicity has been well reported in patients receiving older generations of nucleotide analogues, namely adefovir dipivoxil and tenofovir disoproxil fumarate (TDF). (medscape.com)
- These agents are classified according to their chemical structures: the three nucleoside analogues include lamivudine, telbivudine and entecavir, whereas the two nucleotide analogues include adefovir dipivoxil, tenofovir disoproxil fumarate (TDF), [ 2 ] and the newly approved tenofovir alafenamide (TAF). (medscape.com)
Lamivudine4
- ViiV Healthcare, the global specialist HIV company, majority owned by GlaxoSmithKline, with Pfizer Inc. and Shionogi Limited as shareholders, today announced that the European Commission has granted Marketing Authorisation for Dovato (dolutegravir/lamivudine) for the treatment of HIV-1 infection in adults and adolescents above 12 years of age weighing at least 40 kg, with no known or suspected resistance to the integrase inhibitor class, or lamivudine. (gsk.com)
- Dovato (dolutegravir 50 mg/ lamivudine 300 mg tablets) is authorised in the EU for the treatment of HIV-1 infection in adults and adolescents above 12 years of age weighing at least 40 kg, with no known or suspected resistance to the integrase inhibitor class, or lamivudine. (gsk.com)
- Lamivudine is a potent nucleoside analog reverse transcriptase inhibitor, used for treatment of chronic HBV and HIV/AIDS. (bioservuk.com)
- 1] Lamivudine and Penciclovir inhibits duck hepatitis B virus (DHBV) replication to a comparable extent when used alone, and in combination, the two nucleoside analogs acts synergistically over a wide range of clinically relevant concentrations. (bioservuk.com)
Protease inhibitor2
- Insulin resistance (IR) is common in HIV-seropositive patients, particularly among those receiving protease inhibitor (PI) and is more prevalent among those with lipoatrophy or fat accumulation in the visceral region. (bvsalud.org)
- HAART is defined as a treatment regimen for HIV infection that consists of three drugs, including two nucleoside analogue reverse transcriptase inhibitors combined with either a nonnucleoside reverse transcriptase inhibitor or a protease inhibitor. (cdc.gov)
NNRTIs4
- Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are highly selective for HIV-1 but do not exhibit activity against other viruses. (antimicrobe.org)
- NNRTIs bind noncompetitively to an active site of the reverse transcriptase molecule. (antimicrobe.org)
- Resistance of NNRTIs occurs through mutations of the reverse transcriptase gene in the viral genome. (antimicrobe.org)
- 13 this represents one of two nucleoside analogue reverse transcriptase inhibitors (nnrtis). (surgicalimpex.com)
Integrase strand transfer inhibitors1
- TAFFIC Tablet combines integrase strand transfer inhibitors and nucleoside, nucleotide analog reverse transcriptase inhibitors. (24x7pharma.com)
Stavudine3
- The association between hyperlactatemia and stavudine with or without didanosine was not biased by these medications being more recently available and, therefore, being given preferentially to patients who had prolonged use of nucleoside analog reverse-transcriptase inhibitors. (unige.ch)
- Zerit contains active ingredient stavudine, which is a nucleoside analog reverse transcriptase inhibitor (NARTI) which is active against HIV. (grantpharmacy.com)
- Stavudine triphosphate inhibits the HIV reverse transcriptase by competing with natural substrate, thymidine triphosphate. (grantpharmacy.com)
Regimens4
- Triple nucleoside-only regimens: Early virologic failure has been reported in HIV-infected patients. (nih.gov)
- and studies sponsored by the National Institutes of Health's Adult AIDS Clinical Trials Group for patients who have failed triple combination regimens or treatment with protease inhibitors (ACTG 359 and ACTG 372). (gilead.com)
- Nucleoside analogue reverse transcriptase inhibitors are an integral component of combination antiretroviral treatment regimens. (northwestern.edu)
- The mean time on ART was 75.5 months (95% confidence interval [CI]: 69.0-81.9 months), and 93.7% of the patients were receiving non-nucleoside reverse transcriptase inhibitor-based regimens. (who.int)
Nucleotide analog1
Carbocyclic nucleoside2
- This thesis describes the syntheses of various potential inhibitors of HIV, e.g. some 3´-hydroxymethyl-substituted carbocyclic nucleoside analogues as reverse transcriptase inhibitors and some symmetry-based peptidomimetics as protease inhibitors. (avhandlingar.se)
- Chemically, it is a synthetic carbocyclic nucleoside and is the enantiomer with 1S, 4R absolute configuration on the cyclopentene ring. (newedgeoverseas.com)
Antiviral Activity1
- A deoxycytidine analog and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B viruses. (bvsalud.org)
Regimen2
- TROGARZO, a CD4-directed post-attachment HIV-1 inhibitor, in combination with other antiretroviral(s), is indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in heavily treatment-experienced adults with multidrug resistant HIV-1 infection failing their current antiretroviral regimen. (nih.gov)
- HAART1 regimen (one non-nucleoside reverse transcriptase inhibitor or boosted old protease inhibitors) (HR = 1.94). (biomedcentral.com)
Antiretrovirals1
- Applications: Abacavir is an antiviral nucleoside reverse transcriptase inhibitor used in combination with other antiretrovirals for the treatment of HIV. (newedgeoverseas.com)
Structurally1
- In this work, we employed high-throughput virtual screening (HTVS) to identify potential small molecule Eg5 inhibitors from a designed set of novel dihydropyrimidine analogs structurally similar to monastrol. (emerginginvestigators.org)
AIDS1
- For example, azidothymidine (AZT) is a nucleoside analogue used to prevent and treat HIV/AIDS. (wikipedia.org)
Inhibition1
Synthesis2
- Synthesis pathways differ depending on the specific nucleoside triphosphate being made, but given the many important roles of nucleoside triphosphates, synthesis is tightly regulated in all cases. (wikipedia.org)
- Given their importance in the cell, the synthesis and degradation of nucleoside triphosphates is under tight control. (wikipedia.org)
Enzyme2
- These drugs block the reverse transcriptase enzyme. (aids.org)
- Regarding the family, it is grouped within the Retroviridae family, viruses that have the enzyme Reverse Transcriptase (TR) - responsible for transcribing the RNA genome into complementary DNA (cDNA), being the subfamily Orthoretrovirinae ( 2 ). (scielo.sa.cr)
Monotherapy1
- When nonnucleoside reverse transcriptase inhibitors are used as monotherapy for HIV-1 infection, drug resistance develops rapidly. (antimicrobe.org)
Substrate1
- Lamivudine's anti- HBV activity, like its anti-HIV activity, has been shown to depend on the ability of LMV-TP to serve as both substrate and inhibitor of the DNA- and RNA-dependent polymerase activities of the HBV P gene product. (bioservuk.com)
Genome1
- reverse transcription of the RNA pre-genome takes place within the completed capsid, the protein shell of the core. (grantome.com)
Triphosphate3
- A nucleoside triphosphate is a nucleoside containing a nitrogenous base bound to a 5-carbon sugar (either ribose or deoxyribose), with three phosphate groups bound to the sugar. (wikipedia.org)
- The carbons of the sugar in a nucleoside triphosphate are numbered around the carbon ring starting from the original carbonyl of the sugar. (wikipedia.org)
- This section focuses on nucleoside triphosphate metabolism in humans, but the process is fairly conserved among species. (wikipedia.org)
Hepatitis3
- It works by blocking the HIV reverse transcriptase and hepatitis B virus polymerase . (bioservuk.com)
- Background Safety profile of nucleos(t)ide analogues is an important issue in view of its widespread use for decades in patients with chronic hepatitis B (CHB). (medscape.com)
- The development of oral anti-viral treatment with nucleos(t)ide analogues (NAs) has revolutionised the management of chronic hepatitis B (CHB) in the last two decades. (medscape.com)
Transcription3
- It can readily be embedded in extended models of the complete HIV-1 reverse transcription process, or analogous processes in other viruses and help to guide drug development and improve our understanding of the mechanisms of resistance development during treatment. (plos.org)
- 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)
Nucleotides2
- Nucleotides are nucleosides covalently linked to one or more phosphate groups. (wikipedia.org)
- To provide information about the number of phosphates, nucleotides may instead be referred to as nucleoside (mono, di, or tri) phosphates. (wikipedia.org)
Viral infections3
- Nucleoside analogues may also be used to treat viral infections. (wikipedia.org)
- Nucleoside analogs ( NA s) are used to treat numerous viral infections and cancer. (plos.org)
- Nucleoside analogs ( NA s) represent an important drug class for the treatment of viral infections and cancer. (plos.org)
Efficacy1
Cellular1
- Nucleoside triphosphates also serve as a source of energy for cellular reactions and are involved in signalling pathways. (wikipedia.org)
Toxicity2
- Bone toxicity is closely related to nucleoside analogue effect on renal proximal tubular and phosphaturia. (medscape.com)
- Although NAs are generally safe and relatively free of major side effects, [ 10 ] nephrotoxicity and bone toxicity may occur in a small yet significant proportion of patients receiving older generations of nucleotide analogues, for example, adefovir and TDF. (medscape.com)
Combination1
- Ongoing Clinical Program - PREVEON is currently being studied in late-stage clinical trials for the treatment of HIV in combination with other commercially available antiretroviral therapies, including protease inhibitors. (gilead.com)
Affinity1
- In this study, the authors use high-throughput virtual screening to design and evaluate a set of non-nucleoside reverse transcriptase inhibitors for binding affinity to the protein reverse transcriptase. (emerginginvestigators.org)
Derivatives2
- Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors. (neb.com)
- Carbohydrates so far synthesized are sugers (L-nucleosides, etc.), deoxyamino sugars and their derivatives (D-ManNAc, zanamivir-related sialic acids), and oligosaccharides, such as LeX. (keio.ac.jp)
Patients3
- In patients with early Parkinson's disease, selegiline and other drugs in a class called monoamine oxidase type B inhibitors are cheap and effective treatments that reduce disability and the need for levodopa, researchers reported in the British Medical Journal. (digitalnaturopath.com)
- The focus of our project is to create synthetic aptamers using specialized DNA or RNA bases to act as competitive inhibitors for PLD1 allowing patients to continue chemotherapy. (asdrp.org)
- Yet risks of renal failure and renal replacement therapy were similar in patients treated with nucleoside analogues versus nucleotide analogues in real-life setting. (medscape.com)
Class3
- The table contains 195 products whose active ingredient are classified under the same pharmacologic class Human Immunodeficiency Virus Nucleoside Analog Reverse Transcriptase Inhibitor [EPC]. (ndclist.com)
- And for Parkinson's disease, Hoffman-LaRoche developed Tasmar, the first in a new class of drugs called COMT inhibitors. (pharmexec.com)
- It was the first in a new class of phosphodiesterase type 5 inhibitors. (pharmexec.com)
Drugs1
- The drugs were from at least two different classes the newest one was called protease inhibitors. (hivtalk.net)
Ziagen1
- Ziagen, a Glaxo Wellcome product, was the first new nucleoside analogue reverse transcriptase inhibitor to be approved in more than three years. (pharmexec.com)
Chronic1
- Abbott Laboratories developed Zemplar, the first vitamin D analog to prevent and treat secondary hyperparathyroidism associated with chronic renal failure. (pharmexec.com)
Synthetic1
- Development of synthetic aptamers for use as low-cost PLD1 inhibitors. (asdrp.org)
Commonly1
- Annual inuenza vaccinations are not characteristic of either normal or improvement of flank pain and stiffness in thoracic cage means that clinical judgment and surgical adolescent problems menopause problemspresentation of sexual arousal guanylyl cyclase gtp 5'-gmp detumescence erection pde-8 pde-5 inhibitors are commonly associated with predominant diverticular disease. (surgicalimpex.com)
Treat1
- PREVEON, formerly referred to as adefovir dipivoxil or GS 840, is an investigational, orally-administered, once-daily, reverse transcriptase inhibitor currently being studied in a variety of late-stage clinical studies to treat human immunodeficiency virus (HIV) and prevent cytomegalovirus disease. (gilead.com)
Cases1
- Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogs, including VIREAD. (nih.gov)
Type1
- Thus, nucleoside triphosphates are a type of nucleotide. (wikipedia.org)
Viruses1
- Reverse genetics, the generation of influenza viruses from cDNA, presents a rapid method for creating vaccine strains. (tno.nl)
Methods1
- Methods Relevant articles related to nucleoside analogue safety were selected for review following extensive language- and date-unrestricted, electronic searches of the literature. (medscape.com)
Safety3
- Aim To review and evaluate the latest evidence on the safety profiles of the six approved nucleoside analogues. (medscape.com)
- Conclusions Long-term safety profile of nucleoside analogues is now better defined with more data from large real-life cohorts and clinical trials with long-term follow-up. (medscape.com)
- The new nucleotide analogue, TAF is now available with favourable renal and bone safety profiles. (medscape.com)