Carbon-containing phosphonic acid compounds. Included under this heading are compounds that have carbon bound to either OXYGEN atom or the PHOSPHOROUS atom of the (P=O)O2 structure.
Americium. A completely man-made radioactive actinide with atomic symbol Am, atomic number 95, and atomic weight 243. Its valence can range from +3 to +6. Because of its nonmagnetic ground state, it is an excellent superconductor. It is also used in bone mineral analysis and as a radiation source for radiotherapy.
Compounds having the nitro group, -NO2, attached to carbon. When attached to nitrogen they are nitramines and attached to oxygen they are NITRATES.
Toxic, volatile, flammable liquid hydrocarbon byproduct of coal distillation. It is used as an industrial solvent in paints, varnishes, lacquer thinners, gasoline, etc. Benzene causes central nervous system damage acutely and bone marrow damage chronically and is carcinogenic. It was formerly used as parasiticide.
Organic salts of cyanic acid containing the -OCN radical.
Organic compounds that contain phosphorus as an integral part of the molecule. Included under this heading is broad array of synthetic compounds that are used as PESTICIDES and DRUGS.
A reverse transcriptase inhibitor and ZALCITABINE analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat HIV disease.
A purine base and a fundamental unit of ADENINE NUCLEOTIDES.
The type species of the genus ORTHOHEPADNAVIRUS which causes human HEPATITIS B and is also apparently a causal agent in human HEPATOCELLULAR CARCINOMA. The Dane particle is an intact hepatitis virion, named after its discoverer. Non-infectious spherical and tubular particles are also seen in the serum.
INFLAMMATION of the LIVER in humans caused by HEPATITIS B VIRUS lasting six months or more. It is primarily transmitted by parenteral exposure, such as transfusion of contaminated blood or blood products, but can also be transmitted via sexual or intimate personal contact.
Agents used in the prophylaxis or therapy of VIRUS DISEASES. Some of the ways they may act include preventing viral replication by inhibiting viral DNA polymerase; binding to specific cell-surface receptors and inhibiting viral penetration or uncoating; inhibiting viral protein synthesis; or blocking late stages of virus assembly.
The ability of viruses to resist or to become tolerant to chemotherapeutic agents or antiviral agents. This resistance is acquired through gene mutation.
An opportunistic viral infection of the central nervous system associated with conditions that impair cell-mediated immunity (e.g., ACQUIRED IMMUNODEFICIENCY SYNDROME and other IMMUNOLOGIC DEFICIENCY SYNDROMES; HEMATOLOGIC NEOPLASMS; IMMUNOSUPPRESSION; and COLLAGEN DISEASES). The causative organism is JC Polyomavirus (JC VIRUS) which primarily affects oligodendrocytes, resulting in multiple areas of demyelination. Clinical manifestations include DEMENTIA; ATAXIA; visual disturbances; and other focal neurologic deficits, generally progressing to a vegetative state within 6 months. (From Joynt, Clinical Neurology, 1996, Ch26, pp36-7)
Reproducible depletion of CD4+ lymphocytes below 300 per cubic millimeter in the absence of HIV infection or other known causes of immunodeficiency. This is a rare, heterogeneous syndrome and does not appear to be caused by a transmissible agent.
A species of POLYOMAVIRUS, originally isolated from the brain of a patient with progressive multifocal leukoencephalopathy. The patient's initials J.C. gave the virus its name. Infection is not accompanied by any apparent illness but serious demyelinating disease can appear later, probably following reactivation of latent virus.
Reduction in the number of lymphocytes.
An infection caused by an organism which becomes pathogenic under certain conditions, e.g., during immunosuppression.
Infections with POLYOMAVIRUS, which are often cultured from the urine of kidney transplant patients. Excretion of BK VIRUS is associated with ureteral strictures and CYSTITIS, and that of JC VIRUS with progressive multifocal leukoencephalopathy (LEUKOENCEPHALOPATHY, PROGRESSIVE MULTIFOCAL).
A watery fluid that is continuously produced in the CHOROID PLEXUS and circulates around the surface of the BRAIN; SPINAL CORD; and in the CEREBRAL VENTRICLES.
Decisions made by the United States Supreme Court.
The fraudulent misrepresentation of the diagnosis and treatment of disease.
Facilities or services which are especially devoted to providing palliative and supportive care to the patient with a terminal illness and to the patient's family.
Legal guarantee protecting the individual from attack on personal liberties, right to fair trial, right to vote, and freedom from discrimination on the basis of race, color, religion, sex, age, disability, or national origin. (from http://www.usccr.gov/ accessed 1/31/2003)
Time period from 1901 through 2000 of the common era.
A trace element with the atomic symbol Ni, atomic number 28, and atomic weight 58.69. It is a cofactor of the enzyme UREASE.
A plant family in the order Sapindales that grows in warmer regions and has conspicuous flowers.
A plant family of the order Arales, subclass Arecidae, class Liliopsida (monocot). Many members contain OXALIC ACID and calcium oxalate (OXALATES).
The custard-apple plant family of the order Magnoliales, subclass Magnoliidae, class Magnoliopsida. Some members provide large pulpy fruits and commercial timber. Leaves and wood are often fragrant. Leaves are simple, with smooth margins, and alternately arranged in two rows along the stems.
A family of F-box domain proteins that contain sequences that are homologous to the beta subunit of transducin (BETA-TRANSDUCIN). They play an important role in the protein degradation pathway by becoming components of SKP CULLIN F-BOX PROTEIN LIGASES, which selectively act on a subset of proteins including beta-catenin and IkappaBbeta.
A plant family of the order Violales, subclass Dilleniidae, class Magnoliopsida that are herbaceous or woody vines, shrubs, and trees, mostly of warm regions. Many have tendrils in leaf axils. Leaves are alternate. Flowers have 3-5 sepals, petals and stamens. Nearly all species have seeds that bear a fleshy appendage called an aril.
A plant genus of the family CLUSIACEAE. Members contain XANTHONES.
Compounds that provide LUBRICATION between surfaces in order to reduce FRICTION.
Exclusive legal rights or privileges applied to inventions, plants, etc.
Inhibits the cytotoxic action of quartz and is reported to have delayed the development of experimental silicosis in rats.
The gradual destruction of a metal or alloy due to oxidation or action of a chemical agent. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
Naturally occurring complex liquid hydrocarbons which, after distillation, yield combustible fuels, petrochemicals, and lubricants.

Activation of stimulus-specific serine esterases (proteases) in the initiation of platelet secretion. I. Demonstration with organophosphorus inhibitors. (1/1594)

The effect of organophosphorus inhibitors of serine esterases (proteases) on secretion from washed rabbit platelets was examined. Five noncytotoxic stimuli were employed: collagen, thrombin, heterologous anti-platelet antibody (in the absence of complement), rabbit C3 bound to zymosan, and platelet activating factor derived from antigen-stimulated, IgE-sensitized rabbit basophils. Diisoprophyl phosphofluoridate, three series of p-nitrophenyl ethyl phosphonates, and a series of cyclohexyl phenylalkylphosphonofluridates were all found to be inhibitory to the platelet secretion. These are irreversible inhibitors of serine proteases but in this system were only inhibitory if added to the platelets concurrently with the stimuli. Pretreatment of either the platelets or the stimuli with the inhibitors followed by washing, was without effect on the subsequent reaction. This suggested the involvement of stimulus-activatable serine proteases in the secretory process. The concept was supported by finding that nonphosphorylating phosphonates or hydrolyzed phosphonates or phosphonofluoridates were without inhibitory action. The effect of a series of phosphonates or phosphonoflouridates in inhibiting each stimulus exhibited a unique activity-structure profile. The demonstration of such unique profiles with four series of inhibitors for each of the five stimuli was interpreted as demonstrating that a specific activatable serine protease was involved in the platelet secretory response to each stimulus.  (+info)

Comparative study of the anti-human cytomegalovirus activities and toxicities of a tetrahydrofuran phosphonate analogue of guanosine and cidofovir. (2/1594)

Cidofovir is the first nucleoside monophosphate analogue currently being used for the treatment of human cytomegalovirus (HCMV) retinitis in individuals with AIDS. Unfortunately, the period of therapy with the use of this compound may be limited due to the possible emergence of serious irreversible nephrotoxic effects. New drugs with improved toxicity profiles are needed. The goal of this study was to investigate the anticytomegaloviral properties and drug-induced toxicity of a novel phosphonate analogue, namely, (-)-2-(R)-dihydroxyphosphinoyl-5-(S)-(guanin-9'-yl-methyl) tetrahydrofuran (compound 1), in comparison with those of cidofovir. The inhibitory activities of both compounds on HCMV propagation in vitro were similar against the AD 169 and Towne strains, with 50% inhibitory concentrations ranging from 0.02 to 0.17 microgram/ml for cidofovir and < 0.05 to 0.09 microgram/ml for compound 1. A clinical HCMV isolate that was resistant to ganciclovir and that had a known mutation within the UL54 DNA polymerase gene and a cidofovir-resistant laboratory strain derived from strain AD 169 remained sensitive to compound 1, whereas their susceptibilities to ganciclovir and cidofovir were reduced by 33- and 10-fold, respectively. Both compound 1 and cidofovir exhibited equal potencies in an experimentally induced murine cytomegalovirus (MCMV) infection in mice, with a prevention or prolongation of mean day to death at dosages of 1.0, 3.2, and 10.0 mg/kg of body weight/day. In cytotoxicity experiments, compound 1 was found to be generally more toxic than cidofovir in cell lines Hs68, HFF, and 3T3-L1 (which are permissive for HCMV or MCMV replication) but less toxic than cidofovir in MRC-5 cells (which are permissive for HCMV replication). Drug-induced toxic side effects were noticed for both compounds in rats and guinea pigs in a 5-day repeated-dose study. In guinea pigs, a greater weight loss was noticed with cidofovir than with compound 1 at dosages of 3.0 and 10.0 mg/kg/day. An opposite effect was detected in rats, which were treated with the compounds at relatively high dosages (up to 100 mg/kg/day). Compound 1 and cidofovir were nephrotoxic in both rats and guinea pigs, with the epithelium lining the proximal convoluted tubules in the renal cortex being the primary target site. The incidence and the severity of the lesions were found to be dose dependent. The lesions observed were characterized by cytoplasm degeneration and nuclear modifications such as karyomegaly, the presence of pseudoinclusions, apoptosis, and degenerative changes. In the guinea pig model, a greater incidence and severity of lesions were observed for cidofovir than for compound 1 (P < 0.001) with a drug regimen of 10 mg/kg/day.  (+info)

Impact of 9-(2-phosphonylmethoxyethyl)adenine on (deoxy)ribonucleotide metabolism and nucleic acid synthesis in tumor cells. (3/1594)

Following exposure to 9-(2-phosphonylmethoxyethyl)adenine (an inhibitor of the cellular DNA polymerases alpha, delta and epsilon), human erythroleukemia K562, human T-lymphoid CEM and murine leukemia L1210 cells markedly accumulated in the S phase of the cell cycle. In contrast to DNA replication, RNA synthesis (transcription) and protein synthesis (mRNA translation) were not affected by 9-(2-phosphonylmethoxyethyl)-adenine. The ribonucleoside triphosphate pools were slightly elevated, while the intracellular levels of all four deoxyribonucleoside triphosphates were 1.5-4-fold increased in 9-(2-phosphonylmethoxyethyl)adenine-treated K562, CEM and L1210 cells. The effect of 9-(2-phosphonylmethoxyethyl)adenine on de novo (thymidylate synthase-mediated) and salvage (thymidine kinase-mediated) dTTP synthesis was investigated using radio-labelled nucleoside precursors. The amount of thymidylate synthase-derived dTTP in the acid soluble pool was 2-4-fold higher in PMEA-treated than in untreated K562 cells, which is in accord with the 3-4-fold expansion of the global dTTP level in the presence of 9-(2-phosphonylmethoxyethyl)adenine. Strikingly, 2-derived dTTP accumulated to a much higher extent (i.e. 16-40-fold) in the soluble dTTP pool upon 9-(2-phosphonylmethoxyethyl)adenine treatment. In keeping with this finding, a markedly increased thymidine kinase activity could be demonstrated in extracts of 9-(2-phosphonylmethoxyethyl)adenine-treated K562 cell cultures. Also, in the presence of 200 microM 9-(2-phosphonylmethoxyethyl)adenine, 14-fold less thymidylate synthase-derived but only 3-fold less thymidine kinase-derived dTTP was incorporated into the DNA of the K562 cells. These data show that thymidine incorporation may be inappropriate as a cell proliferation marker in the presence of DNA synthesis inhibitors such as 9-(2-phosphonylmethoxyethyl)adenine. Our findings indicate that 9-(2-phosphonylmethoxyethyl)adenine causes a peculiar pattern of (deoxy)ribonucleotide metabolism deregulation in drug-treated tumor cells, as a result of the metabolic block imposed by the drug on the S phase of the cell cycle.  (+info)

Early short-term 9-[2-(R)-(phosphonomethoxy)propyl]adenine treatment favorably alters the subsequent disease course in simian immunodeficiency virus-infected newborn Rhesus macaques. (4/1594)

Simian immunodeficiency virus (SIV) infection of newborn macaques is a useful animal model of human pediatric AIDS to study disease pathogenesis and to develop intervention strategies aimed at delaying disease. In the present study, we demonstrate that very early events of infection greatly determine the ultimate disease course, as short-term antiviral drug administration during the initial viremia stage significantly delayed the onset of AIDS. Fourteen newborn macaques were inoculated orally with uncloned, highly virulent SIVmac251. The four untreated control animals showed persistently high virus levels and poor antiviral immune responses; they developed fatal immunodeficiency within 15 weeks. In contrast, SIV-infected newborn macaques which were started on 9-[2-(R)-(phosphonomethoxy)propyl]adenine (PMPA) treatment at 5 days of age and continued for either 14 or 60 days showed reduced virus levels and enhanced antiviral immune responses. This short-term PMPA treatment did not induce detectable emergence of SIV mutants with reduced in vitro susceptibility to PMPA. Although viremia increased in most animals after PMPA treatment was withdrawn, all animals remained disease-free for at least 6 months. Our data suggest that short-term treatment with a potent antiviral drug regimen during the initial viremia will significantly prolong AIDS-free survival for HIV-infected infants and adults.  (+info)

9-[2-(Phosphonomethoxy)propyl]adenine (PMPA) therapy prolongs survival of infant macaques inoculated with simian immunodeficiency virus with reduced susceptibility to PMPA. (5/1594)

Simian immunodeficiency virus (SIV) infection of newborn rhesus macaques is a useful animal model of human immunodeficiency virus infection for the study of the emergence and clinical implications of drug-resistant viral mutants. We previously demonstrated that SIV-infected infant macaques receiving prolonged treatment with 9-[2-(phosphonomethoxy)propyl]adenine (PMPA) developed viral mutants with fivefold reduced susceptibility to PMPA in vitro and that the development of these mutants was associated with the development of a K65R mutation and additional compensatory mutations in reverse transcriptase (RT). To study directly the virulence and clinical implications of these SIV mutants, two uncloned SIVmac isolates with similar fivefold reduced in vitro susceptibilities to PMPA but distinct RT genotypes, SIVmac055 (K65R, N69T, R82K A158S,S211N) and SIVmac385 (K65R, N69S, I118V), were each inoculated intravenously into six newborn rhesus macaques; 3 weeks later, three animals of each group were started on PMPA treatment. All six untreated animals developed persistently high levels of viremia and fatal immunodeficiency within 4 months. In contrast, the six PMPA-treated animals, despite having persistently high virus levels, survived significantly longer: 5 to 9 months for the three SIVmac055-infected infants and > or = 21 months for the three SIVmac385-infected infants. Virus from only one untreated animal demonstrated reversion to wild-type susceptibility and loss of the K65R mutation. In several other animals, additional RT mutations, including K64R and Y115F, were detected, but the biological role of these mutations is unclear since they did not affect the in vitro susceptibility of the virus to PMPA. In conclusion, this study demonstrates that although SIVmac mutants with the PMPA-selected K65R mutation in RT were highly virulent, PMPA treatment still offered strong therapeutic benefits. These results suggest that the potential emergence of HIV mutants with reduced susceptibility to PMPA in patients during prolonged PMPA therapy may not eliminate its therapeutic benefits.  (+info)

Phase I study of combination therapy with intravenous cidofovir and oral ganciclovir for cytomegalovirus retinitis in patients with AIDS. (6/1594)

Ganciclovir and cidofovir, two antiviral agents used in the treatment of cytomegalovirus (CMV) retinitis, have a synergistic effect inhibiting CMV replication in vitro. In a phase I study, seven patients with AIDS-related CMV retinitis were treated with cidofovir (5 mg/kg intravenously every 2 weeks) combined with ganciclovir (1 g orally three times a day). During a median of 5.5 months (range, 1-12 months) of combined therapy, only one patient had retinitis progression, and only two of 28 blood cultures (specimens of which were obtained on a monthly basis) yielded CMV. Dose-limiting adverse ocular effects (anterior uveitis [two patients] and hypotony [two patients]) occurred in three of seven patients. The results suggest that combination therapy with intravenous cidofovir and oral ganciclovir (a regimen that does not require indwelling central venous catheter access) might enhance clinical efficacy. Less frequent administration of cidofovir in combination with oral ganciclovir should be prospectively studied to determine if the incidence of treatment-associated toxicity might be reduced.  (+info)

Actions of 3-[2-phosphonomethyl[1,1-biphenyl]-3-yl]alanine (PMBA) on cloned glycine receptors. (7/1594)

1. PMBA is a novel antagonist of strychnine-sensitive glycine receptors in the rat spinal cord, however, its mode of action is unknown. The actions of PMBA on rat glycine receptor alpha1 and alpha2 homomers in Xenopus oocytes were studied under two-electrode voltage-clamp. 2. Co-application of PMBA and glycine to both alpha1 and alpha2 homomers yielded inward currents which decayed to a steady-state. Responses rose slowly to the same steady-state amplitude following a 2 min pre-incubation in PMBA. Strychnine, but not picrotoxinin, showed similar antagonism to PMBA. The potency of PMBA was independent of membrane potential between -100 and 0 mV. 3. When tested against EC50 concentrations of glycine, PMBA was almost equally potent on alpha1 (IC50, 406+/-41 nM: Hill coefficient, 1.5+/-0.2) and alpha2 (IC50, 539+/-56 nM; Hill coefficient, 1.4+/-0.2) homomers. 4. PMBA (1-I0 microM) and strychnine (200 nM) reduced the potency of glycine and the amplitude of the maximal agonist response of alpha1 and alpha2 homomers. In 10 microM PMBA, two distinct classes of glycine response were observed on alpha2, only a single class of responses were observed on alpha1. 5. There are similarities in PMBA and strychnine antagonism, although these compounds are structurally distinct. The possibility that PMBA interacts at two binding sites which differ in alpha1 and alpha2 subunits is discussed. PMBA may provide a lead structure for novel antagonists with which to investigate structural differences in glycine receptor at alpha1 and alpha2 subunits.  (+info)

Fluorescein monophosphates as fluorogenic substrates for protein tyrosine phosphatases. (8/1594)

A series of novel fluorescein monophosphates aimed as substrates for protein tyrosine phosphatases (PTPs) were synthesized and evaluated against fluorescein diphosphate (FDP), the currently used fluorescent substrate for PTPs. In contrast to FDP, which is dephosphorylated to monophosphate and then to fluorescein in a sequential reaction, these monophosphates are dephosphorylated in a single step. This eliminates the complication in assaying PTPs due to the cleavage of the second phosphate group. The kinetic studies of these substrates with PTPs were performed and Michaelis-Menten parameters were obtained. These designed substrates have Km 0.03-0. 35 mM, kcat/Km of 3-100 mM-1 s-1 with CD45 and PTP1B. The results showed that the substrates with negative charge groups on the fluorescein have higher affinities for PTP1B, which are consistent with other observations. In this series, fluorescein monosulfate monophosphate (FMSP) was the best substrate observed. Since FMSP showed large increases in both absorption and fluorescence upon dephosphorylation by PTPs at pH>6.0, it is one of the most sensitive, stable and high affinity substrates reported for PTPs.  (+info)

2015 Elsevier Ltd. Background Tenofovir disoproxil fumarate can cause renal and bone toxic effects related to high plasma tenofovir concentrations. Tenofovir alafenamide is a novel tenofovir prodrug with a 90% reduction in plasma tenofovir concentrations. Tenofovir alafenamide-containing regimens can have improved renal and bone safety compared with tenofovir disoproxil fumarate-containing regimens. Methods In these two controlled, double-blind phase 3 studies, we recruited treatment-naive HIV-infected patients with an estimated creatinine clearance of 50 mL per min or higher from 178 outpatient centres in 16 countries. Patients were randomly assigned (1:1) to receive once-daily oral tablets containing 150 mg elvitegravir, 150 mg cobicistat, 200 mg emtricitabine, and 10 mg tenofovir alafenamide (E/C/F/tenofovir alafenamide) or 300 mg tenofovir disoproxil fumarate (E/C/F/tenofovir disoproxil fumarate) with matching placebo. Randomisation was done by a computer-generated allocation sequence (block ...
Emtricitabine/tenofovir disoproxil fumarate drug information: uses, indications, side effects, dosage. Compare prices for generic emtricitabine/tenofovir disoproxil fumarate substitutes: Emtricitabine and Tenofovir Tablets, Tavin- EM, Tenof- EM
Lamivudine and tenofovir disoproxil fumarate - Get up-to-date information on Lamivudine and tenofovir disoproxil fumarate side effects, uses, dosage, overdose, pregnancy, alcohol and more. Learn more about Lamivudine and tenofovir disoproxil fumarate
TY - JOUR. T1 - Randomized trial of emtricitabine/tenofovir disoproxil fumarate after hepatitis B immunoglobulin withdrawal after liver transplantation. AU - Teperman, Lewis W.. AU - Poordad, Fred. AU - Bzowej, Natalie. AU - Martin, Paul. AU - Pungpapong, Surakit. AU - Schiano, Thomas. AU - Flaherty, John. AU - Dinh, Phillip. AU - Rossi, Stephen. AU - Subramanian, G. Mani. AU - Spivey, James. N1 - Copyright: Copyright 2013 Elsevier B.V., All rights reserved.. PY - 2013/6. Y1 - 2013/6. N2 - Long-term prophylaxis with hepatitis B immunoglobulin (HBIG) for the prevention of hepatitis B virus (HBV) recurrence after orthotopic liver transplantation (OLT) in patients with chronic HBV infection is inconvenient and costly. This randomized, prospective phase 2 study compared emtricitabine (FTC)/tenofovir disoproxil fumarate (TDF) after HBIG withdrawal to FTC/TDF plus HBIG for the prevention of HBV recurrence after OLT. Forty patients with a median time since liver transplantation of 3.4 years ...
TY - JOUR. T1 - Long-term (96-week) Efficacy and Safety After Switching from Tenofovir Disoproxil Fumarate (TDF) to Tenofovir Alafenamide (TAF) in HIV-infected, Virologically Suppressed Adults. AU - Raffi, Francois. AU - Orkin, Chloe. AU - Clarke, Amanda. AU - Slama, Laurence. AU - Gallant, Joel. AU - Daar, Eric. AU - Henry, Keith. AU - Santana-Bagur, Jorge. AU - Stein, David K.. AU - Bellos, Nicholaos. AU - Scarsella, Anthony. AU - Yan, Mingjin. AU - Abram, Michael E.. AU - Cheng, Andrew. AU - Rhee, Martin S S. PY - 2017/3/6. Y1 - 2017/3/6. N2 - ABSTRACT:: In a double-blind, phase 3 trial, 663 HIV-infected, virologically suppressed adults were randomized to switch to tenofovir alafenamide (TAF; n=333) vs. remain on tenofovir disoproxil fumarate (TDF; n=330), each coformulated with emtricitabine (FTC), while continuing their third agent (boosted protease inhibitor or unboosted third agent). At week 96, 88.6% on FTC/TAF and 89.1% on FTC/TDF had HIV-1 RNA ,50 copies/mL (adjusted difference -0.5%; ...
TY - JOUR. T1 - Tenofovir disoproxil fumarate monotherapy for nucleos(t)ide-naïve chronic hepatitis B patients in Korea. T2 - data from the clinical practice setting in a single-center cohort. AU - Ahn, Sung S.oo. AU - Chon, Young E.un. AU - Kim, Beom K.yung. AU - Kim, Seung U.p.. AU - Kim, Do Y.oung. AU - Ahn, Sang H.oon. AU - Han, Kwang Hyub. AU - Park, Jun Y.ong. PY - 2014/9/1. Y1 - 2014/9/1. N2 - BACKGROUND/AIMS: This study assessed the antiviral efficacy and safety of tenofovir disoproxil fumarate (TDF) for up to 12 months in Korean treatment-naïve chronic hepatitis B (CHB) patients.METHODS: A total of 411 treatment-naïve CHB patients who had been treated with TDF for at least 3 months (median 5.6) were consecutively enrolled. Clinical, biochemical, virological parameters and treatment adherence were routinely assessed every 3 months.RESULTS: The median age was 51.3 years, 63.0% of the patients were male, 49.6% were HBeAg (+), and 210 patients had liver cirrhosis. The median baseline HBV ...
TY - JOUR. T1 - The Lymphoid Tissue Pharmacokinetics of Tenofovir Disoproxil Fumarate and Tenofovir Alafenamide in HIV-Infected Persons. AU - Fletcher, Courtney V.. AU - Podany, Anthony T.. AU - Thorkelson, Ann. AU - Winchester, Lee C.. AU - Mykris, Timothy. AU - Anderson, Jodi. AU - Jorstad, Siri. AU - Baker, Jason V.. AU - Schacker, Timothy W.. N1 - Funding Information: This work was supported by grants 1R01 AI‐124965 (to CVF) and U01 AI‐105872 (to TWS) from the National Institute of Allergy and Infectious Diseases. Publisher Copyright: © 2020 The Authors Clinical Pharmacology & Therapeutics © 2020 American Society for Clinical Pharmacology and Therapeutics. PY - 2020/11/1. Y1 - 2020/11/1. N2 - The secondary lymphoid tissues (LT), lymph nodes (LN) and gut-associated lymphoid tissue are the primary sites of HIV replication and where the latent pool of virus is maintained. We compared the pharmacokinetics of tenofovir disoproxil fumarate (TDF) and tenofovir alafenamide (TAF) in LT of 13 ...
Tenofovir Disoproxil Fumarate(TDF) (CAS 202138-50-9) Market Research Report 2018 aims at providing comprehensive data on tenofovir disoproxil fumarate(tdf)
TY - JOUR. T1 - Infant growth outcomes after maternal tenofovir disoproxil fumarate use during pregnancy.. AU - Ransom, Carla E.. AU - Huo, Yanling. AU - Patel, Kunjal. AU - Scott, Gwendolyn B.. AU - Watts, Heather D.. AU - Williams, Paige. AU - Siberry, George K.. AU - Livingston, Elizabeth G.. PY - 2013/12/1. Y1 - 2013/12/1. N2 - To determine whether maternal use of tenofovir disoproxil fumarate for treatment of HIV in pregnancy predicts fetal and infant growth. The study population included HIV-uninfected live-born singleton infants of mothers enrolled in the International Maternal Pediatric Adolescent AIDS Clinical Trials Group protocol P1025 (born 2002-2011) in the United States and exposed in utero to a combined (triple or more) antiretroviral regimen. Infant weight at birth and 6 months was compared between infants exposed and unexposed to tenofovir in utero using 2-sample t test, χ test, and multivariable linear and logistic regression models, including demographic and maternal ...
A Randomized, Phase II, Controlled Trial Comparing the Efficacy of Adefovir Dipivoxil and Tenofovir Disoproxil Fumarate for the Treatment of Lamivudine-Resistant Hepatitis B Virus in Subjects Who Are Co-Infected With HIV ...
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Tenofovir disoproxil fumarate (TDF) 300 mg plus placebo to match adefovir dipivoxil (ADV) (double-blind period), followed by TDF 300 mg (open-label period). Participants may have added emtricitabine (FTC) to their treatment regimen (as part of FTC 200 mg/TDF 300 mg fixed-dose combination (FDC) tablet) in the open-label period ...
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BACKGROUND: Effective two-drug regimens could decrease long-term drug exposure and toxicity with HIV-1 antiretroviral therapy (ART). We therefore aimed to evaluate the efficacy and safety of a two-drug regimen compared with a three-drug regimen for the treatment of HIV-1 infection in ART-naive adults.. METHODS: We conducted two identically designed, multicentre, double-blind, randomised, non-inferiority, phase 3 trials: GEMINI-1 and GEMINI-2. Both studies were done at 192 centres in 21 countries. We included participants (≥18 years) with HIV-1 infection and a screening HIV-1 RNA of 500 000 copies per mL or less, and who were naive to ART. We randomly assigned participants (1:1) to receive a once-daily two-drug regimen of dolutegravir (50 mg) plus lamivudine (300 mg) or a once-daily three-drug regimen of dolutegravir (50 mg) plus tenofovir disoproxil fumarate (300 mg) and emtricitabine (200 mg). Both drug regimens were administered orally. We masked participants and investigators to treatment ...
This study is to evaluate the steady-state pharmacokinetics (PK) and confirm the dose of the elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate (EVG/COBI/FTC/TDF) single tablet regimen (STR) in HIV-1 infected, antiretroviral (ARV) treatment-naive adolescents. Safety, tolerability, and efficacy will also be evaluated through Week 48.. A total of 50 adolescent participants (12 to , 18 years of age) will be enrolled to receive EVG/COBI/FTC/TDF as follows:. ...
Background: Off-target renal and bone side effects may occur with tenofovir disoproxil fumarate (TDF) use. Compared with TDF, tenofovir alafenamide (TAF) results in significantly reduced plasma tenofovir (TFV) and may have less renal and bone toxicity.. Methods: Treatment naïve HIV-1+ adults were randomized 1:1 to a single tablet regimen of E/C/F/TAF or E/C/F/TDF once daily in two double blind studies. Assessments included measures of renal function and bone mineral density (BMD). Four pre-specified secondary safety endpoints were tested: serum creatinine, treatment-emergent proteinuria, spine and hip BMD. Week 48 off-target side effects data are described.. Results: Combined, the two studies randomized and treated 1,733 subjects. Plasma TFV was ,90% lower (mean [%CV] AUCtau 297 (20) vs. 3,410 (25) nghr/mL) in the E/C/F/TAF arm, compared to the E/C/F/TDF arm. Serum creatinine (mean [SD] change: +0.08 [0.124] vs +0.11 [0.217] mg/dL, p,0.001), quantified proteinuria (UPCR, median [Q1, Q3] % ...
Medication Guide TRUVADA (tru-vah-dah) (emtricitabine and tenofovir disoproxil fumarate) Tablets Read this Medication Guide before you start taking TRUVADA and each time you get a refill. There may be
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Learn about Complera (Emtricitabine/Rilpivirine/Tenofovir Disoproxil Fumarate Tablets) may treat, uses, dosage, side effects, drug interactions, warnings, patient labeling, reviews, and related medications.
Professional guide for Elvitegravir, Cobicistat, Emtricitabine, and Tenofovir Disoproxil Fumarate. Includes: pharmacology, pharmacokinetics, contraindications, interactions, adverse reactions and more.
On June 8, 2017, the Food and Drug Administration approved the first generic version of emtricitabine and tenofovir disoproxil fumarate tablets, ...
This study compared the efficacy and tolerability of entecavir versus tenofovir disoproxil fumarate in patients with chronic hepatitis B.
Brand Name: Cimduo Other Names: 3TC/TDF, Lamivudine/Tenofovir Disoproxil Fumarate Drug Class: Nucleoside Reverse Transcriptase Inhibitors WARNING:Cimduo can cause serious, life-threatening side effec
Background. The efficacy of tenofovir disoproxil fumarate (TDF) as part of combination antiretroviral treatment (ART) has been demonstrated in several randomized, controlled trials. However, an increasing number of case reports suggest that TDF use may be associated with significant nephrotoxicity. Our objective was to determine the renal safety of TDF-containing ART regimens for HIV-infected individuals.. Methods. MEDLINE, EMBASE, Global Health, Scopus, Biosis Previews, Cochrane Library, Web of Science, and existing systematic reviews were searched. Prospective studies comparing TDF-containing with non-TDF containing ART regimens were selected for inclusion. We extracted data on study characteristics, participant characteristics, therapeutic interventions, renal function, bone density, and fracture rates.. Results. A total of 17 studies (including 9 randomized, controlled trials) met the selection criteria. Median sample size was 517 participants. Constituent ART regimens were diverse. There ...
Background: Tenofovir disoproxil fumarate (TDF) is the antiretroviral drug most commonly associated with renal dysfunction. However, few studies have examined this association in sub-Saharan Africa despite recent scale-up of antiretroviral therapy (ART) to all people living wi...
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Lim, S.G., Marcellin, P., Tassopoulos, N., Hadziyannis, S., Chang, T.T., Tong, M., Sievert, W., Hu, P., Arterburn, S., Brosgart, C.L. (2007). Clinical trial: Effects of adefovir dipivoxil therapy in Asian and Caucasian patients with chronic hepatitis B. Alimentary Pharmacology and Therapeutics 26 (10) : 1419-1428. [email protected] Repository. https://doi.org/10.1111/j.1365-2036.2007.03506. ...
Darunavir/cobicistat/emtricitabine/tenofovir alafenamide (D/C/F/TAF) 800/150/200/10 mg is a once-daily, single-tablet regimen for treatment of HIV-1 infection. The efficacy/safety of switching to D/C/F/TAF versus continuing boosted protease inhibitor (bPI) + emtricitabine/tenofovir disoproxil fumarate (control) were demonstrated in a phase 3, randomized study (EMERALD) of treatment-experienced, virologically suppressed adults through week 48. The objective of this analysis was to evaluate EMERALD outcomes across subgroups of patients based on demographic characteristics, prior treatment experience, and baseline antiretroviral regimen. EMERALD patients were virologically suppressed (viral load [VL] | 50 copies/mL for ≥ 2 months at screening). Prior non-darunavir virologic failure (VF) was allowed. Primary endpoint was proportion of patients with virologic rebound (confirmed VL ≥ 50 copies/mL) cumulative through week 48. Virologic response was VL | 50 copies/mL (FDA snapshot). Safety was assessed by
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 ...
Tenofovir disoproxil fumarate: Find the most comprehensive real-world treatment information on Tenofovir disoproxil fumarate at PatientsLikeMe. 48 patients with fibromyalgia, multiple sclerosis, major depressive disorder, generalized anxiety disorder, diabetes type 2, systemic lupus erythematosus, post-traumatic stress disorder, rheumatoid arthritis, Parkinsons disease, bipolar disorder, high blood pressure (hypertension), panic disorder, myalgic encephalomyelitis/chronic fatigue syndrome, amyotrophic lateral sclerosis, persistent depressive disorder (dysthymia), epilepsy, migraine, hypothyroidism, osteoarthritis, high cholesterol (hypercholesterolemia), attention deficit/hyperactivity disorder, bipolar II disorder, asthma, traumatic brain injury, social anxiety disorder, irritable bowel syndrome, chronic obstructive pulmonary disease, idiopathic pulmonary fibrosis, gastroesophageal reflux disease or bipolar I disorder currently take Tenofovir disoproxil fumarate.
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Virologic breakthrough in a patient with chronic hepatitis B by combination treatment with tenofovir disoproxil fumarate and entecavir Fumitaka Suzuki,1,2 Hitomi Sezaki,1 Norio Akuta,1 Yoshiyuki Suzuki,1 Yusuke Kawamura,1 Tetsuya Hosaka,1 Masahiro Kobayashi,1 Satoshi Saitoh,1 Yasuji Arase,1 Kenji Ikeda,1 Mariko Kobayashi,3 Sachiyo Watahiki,3 Rie Mineta,3 Yukiko Suzuki,3 Hiromitsu Kumada1 1Department of Hepatology, Toranomon Hospital, Tokyo, Japan; 2Okinaka Memorial Institute for Medical Research, Tokyo, Japan; 3Research Institute for Hepatology, Toranomon Branch Hospital, Kawasaki, Japan Abstract: Tenofovir disoproxil fumarate (TDF) is widely used to treat hepatitis B virus (HBV) patients in the USA and Europe. No confirmed report of resistance selection during treatment with TDF in treatment-naïve and nucleoside/nucleotide analog-treated chronic hepatitis B patients has yet been reported. Here, we report for the first time a patient with chronic hepatitis B and cirrhosis who emerged with
The Birmingham group described the clinical course of four liver transplant patients who developed graft infection with lamivudine resistant virus. Lamivudine resistant hepatitis B developed after a mean duration of nine months (range 8-11) after the transplant. Liver function abnormalities occurred at a mean duration of six months (range 3-12) after the emergence of lamivudine resistant virus and three of the four patients died 5-20 months later. The authors concluded that the lamivudine resistant phenotype can cause severe graft damage.. In our liver transplant centre, 12 patients with chronic hepatitis B (four with hepatocellular carcinoma) underwent liver transplantation over a five year period. All were given lamivudine before and after transplant. Lamivudine resistant hepatitis B developed in six of the nine survivors at a mean duration of 60 weeks (range 1-127) after liver transplant. Apart from weaning off immunosuppression aggressively, no further antiviral treatment was added. All six ...
Editor,-We read with interest the article by Mutimer and colleagues (Gut2000;46:107-113). The Birmingham group described the clinical course of four liver transplant patients who developed graft infection with lamivudine resistant virus. Lamivudine resistant hepatitis B developed after a mean duration of nine months (range 8-11) after the transplant. Liver function abnormalities occurred at a mean duration of six months (range 3-12) after the emergence of lamivudine resistant virus and three of the four patients died 5-20 months later. The authors concluded that the lamivudine resistant phenotype can cause severe graft damage.. In our liver transplant centre, 12 patients with chronic hepatitis B (four with hepatocellular carcinoma) underwent liver transplantation over a five year period. All were given lamivudine before and after transplant. Lamivudine resistant hepatitis B developed in six of the nine survivors at a mean duration of 60 weeks (range 1-127) after liver transplant. Apart from ...
article{6522cd05-413f-44ab-952b-a598c9530962, abstract = {Reaction of [Re-2(CO)(9)(NCMe)] with tri(2-thienyl)phosphine (PTh3) in refluxing cyclohexane affords three substituted dirhenium complexes: [Re-2(CO)(9)(PTh3)] (1), [Re-2(CO)(8)(NCMe)(PTh3)] (2), and [Re-2(CO)(8)(PTh3)(2)] (3). Complex 2 was also obtained from the room-temperature reaction of [Re-2(CO)(8)(NCMe)(2)] with PTh3 and is an unusual example in which the acetonitrile and phosphine ligands are coordinated to the same rhenium atom. Thermolysis of 1 and 3 in refluxing xylene affords [Re-2(CO)(8)(mu-PTh2)(mu-eta(1):kappa(1)-C4H3S)] (4) and [Re-2(CO)(7)(PTh3)(mu-PTh2)(mu-H)] (5), respectively, both resulting from carbon-phosphorus bond cleavage of a coordinated PTh3 ligand. Reaction of [Re-2(CO)10] and PTh3 in refluxing xylene gives a complex mixture of products. These products include 3-5, two further binuclear products, [Re-2(CO)(7)(PTh3)(mu-PTh2)(mu-eta(1):kappa(1)-C4H3S)] (6) and ...
TY - JOUR. T1 - Synthesis of fluorescent phosphatidylinositols using a novel inositol H- phosphonate. AU - Leung, Lawrence W.. AU - Vilchèze, Catherine. AU - Bittman, Robert. PY - 1998/5/7. Y1 - 1998/5/7. N2 - Coupling of 1,2-diradyl-sn-glycerol 5 with the novel inositol H- phosphonate derivative, 6-O-benzyl-2,3:4,5-di-O-isopropylidene-myo-inositol H-phosphonate (3), gave fluorescent analogs of phosphatidylinositol (PtdIns, 1) and PtdIns(4,5)-bisphosphate (PtdIns(4,5)P2, 2). Unlike the corresponding phosphoramidate, 3 was stable at -20 °C for several months, making it a useful intermediate for the synthesis of myo-inositol phospholipids.. AB - Coupling of 1,2-diradyl-sn-glycerol 5 with the novel inositol H- phosphonate derivative, 6-O-benzyl-2,3:4,5-di-O-isopropylidene-myo-inositol H-phosphonate (3), gave fluorescent analogs of phosphatidylinositol (PtdIns, 1) and PtdIns(4,5)-bisphosphate (PtdIns(4,5)P2, 2). Unlike the corresponding phosphoramidate, 3 was stable at -20 °C for several months, ...
Phosphonic and phosphinic acid are similar to phosphate ester and anhydrides with instead of carbon oxygen bond have the C-P-C bond. They are stable and can stand against harsh chemical treatments. In many cases, phosphorus is a limiting reagent so the discover of about 20-30% of phosphorus in the ocean was an important discovery.. The first naturally produced phosphonate compound was 2-aminoethylphosphonate (AEP). AEP was found in phosphonolipids. Phosphonolipids are present in many protozoa, plants, bacteria and even humans. It was found they are formed through ingestion and not made by the body. These phosphonolipids have a fatty acid chain and different phosphonate headgroups. Observation show that phosphonates affect the metabolism. More studies need to be performed on the function of the macromolecules of phosphonate containing molecules because it is still not understood every well. The synthesis of AEP from phosphonoenolpyruvate PEP, is the shortest known pathway to produce natural ...
See Article on [Related article:] 230. Clinical resistance to tenofovir disoproxil fumarate (TDF) did not develop in any patient after 8 years of TDF treatment in a phase III clinical trial for treatment-naïve patients with chronic hepatitis B (CHB) [1]. Potent efficacy and high barrier to resistance of TDF have been established, even in patients who have been previously treated with nucleos(t)ide analogues (NUCs) or have NUC-resistant hepatitis B virus (HBV) variants. We previously reported that TDF-based rescue therapy was effective in patients harboring lamivudine (LAM)-resistant or multidrug-resistant HBV variants [2,3]. Moreover, two randomized controlled trials evaluating the efficacy of TDF monotherapy in patients infected with HBV variants resistant to adefovir (ADV) and entecavir (ETV) were conducted, and non-inferior antiviral efficacy compared with TDF plus ETV combination therapy was demonstrated [4,5]. On the basis of in vitro and in vivo data, there was concern that HBV ...
Replication stress is a common feature of cancer cells. Ataxia telangiectasia-mutated (ATM) and Rad3-related (ATR) signalling, a DNA damage repair (DDR) pathway, is activated by regions of single-stranded DNA (ssDNA) that can arise during replication stress. ATR delays cell cycle progression and prevents DNA replication fork collapse, which prohibits cell death and promotes proliferation. Several ATR inhibitors have been developed in order to restrain this protective mechanism in tumours. It is known, however, that despite other effective anticancer chemotherapy treatments targeting DDR pathways, resistance occurs. This begets the need to identify combination treatments to overcome resistance and prevent tumour cell growth. We conducted a drug screen to identify potential synergistic combination treatments by screening an ATR inhibitor (VE822) together with compounds from a bioactive small molecule library. The screen identified adefovir dipivoxil, a reverse transcriptase inhibitor and nucleoside
Tenofovir (TFV) is an antiviral drug approved for treating Human Immunodeficiency Virus (HIV) and Hepatitis B. TFV is administered orally as the prodrug tenofovir disoproxil fumarate (TDF) which then is deesterified to the active drug TFV. TFV induces nephrotoxicity characterized by renal failure and Fanconi Syndrome. The mechanism of this toxicity remains unknown due to limited experimental models. This study investigated the cellular mechanism of cytotoxicity using a human renal proximal tubular epithelial cell line (HK-2). HK-2 cells were grown for 48 h followed by 24 to 72 h exposure to 0-28.8 μM TFV or vehicle, phosphate buffered saline (PBS). MTT (MTT, 3-(4,5-dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) and Trypan blue indicated that TFV diminished cell viability at 24-72 h. TFV decreased ATP levels at 72 h when compared to vehicle, reflecting mitochondrial dysfunction. TFV increased the oxidative stress biomarkers of protein carbonylation and 4-hydroxynonenol (4-HNE) adduct formation.
2014 International Medical Press. Background: Tenofovir (TDF) is associated with phosphaturia and elevated 1,25 dihydroxy vitamin D (1,25-OH(2)D). Fibroblast growth factor 23 (FGF23) causes phosphaturia and increases in response to elevated 1,25-OH(2)D. Vitamin D-binding protein (VDBP) binds to 1,25-OH(2)D, decreasing its biological activity, and is elevated in individuals with higher plasma tenofovir concentrations. We compared FGF23 and VDBP before and after vitamin D3 (VITD) supplementation in youths treated with combination antiretroviral therapy (cART) containing or not containing TDF.Methods: A randomized controlled trial in HIV-positive youths aged 18-25 years enrolled participants based on cART treatment with TDF (TDF; n=118) or without TDF (no-TDF; n=85), and randomized within those groups to VITD (50,000 IU every 4 weeks) or placebo (PL). We measured FGF23 and VDBP and calculated free 1,25-OH(2)D at baseline and week 12, and compared changes by TDF treatment and VITD randomized ...
Phosphonates and phosphonic acids are organophosphorus compounds containing C−PO(OH)2 or C−PO(OR)2 groups (where R = alkyl, aryl). Phosphonic acids, typically handled as salts, are generally nonvolatile solids that are poorly soluble in organic solvents, but soluble in water and common alcohols. Many commercially important compounds are phosphonates, including glyphosate, the herbicide Roundup, and ethephon, a widely used plant growth regulator. Bisphosphonates are popular drugs for treatment of osteoporosis. In biology and medicinal chemistry, phosphonate groups are used as stable bioisoteres for phosphate, such as in the antiviral nucleotide analogue, Tenofovir, one of the cornerstones of anti-HIV therapy. Phosphonates feature tetrahedral phosphorus centers. They are structurally closely related to (and often prepared from) phosphorous acid. Phosphonate salts are the result of deprotonation of phosphonic acids, which are diprotic acids: RPO(OH)2 + NaOH → H2O + RPO(OH)(ONa) (monosodium ...
BACKGROUND: Pre-exposure prophylaxis (PrEP) trials using tenofovir-based regimens have demonstrated that high levels of adherence are required to evaluate efficacy; the incorporation of objective biomarkers of adherence in trial design has been essential to interpretation, given the inaccuracy of self-report. Antiretroviral measurements in scalp hair have been useful as a marker of long-term exposure in the HIV treatment setting, and hair samples are relatively easy and inexpensive to collect, transport, and store for analysis. To evaluate the relationship between dose and tenofovir concentrations in hair, we examined the dose proportionality of tenofovir in hair in healthy, HIV-uninfected adults. METHODS: A phase I, crossover pharmacokinetic study was performed in 24 HIV-negative adults receiving directly-observed oral tenofovir tablets administered 2, 4, and 7 doses/week for 6 weeks, with a ≥3-week break between periods. Small samples of hair were collected after each six-week period and analyzed
Ricovir -Em for preventing HIV exposure . You need to know the price of the drug Ricovir -How much? Dont know where Tenofovir 300mg and Emtricitabine 200mg are sold? index-china is the address of buying and selling Ricovir - Em medicine in Ho Chi Minh City, Hanoi, Da Nang, Can Tho ... and nationwide. Ricovir-Em medicine, Tenofovir 300mg and Emtricitabine 200mg against HIV exposure Drug name: Ricovir -Em Ingredients: Tenofovir & Emtricitabine Content: 300mg / 200mg Form: Tablets Package: Box of 30 tablets Production company: Mylan Prices for Ricovir-Emm: COMMENT below for prices OR Click on the link: https://thuoclp.com/chatFB type Ricovir-Em.
In recent decades, researchers have made great efforts to explore alternative biomedical interventions, such as male circumcision (MC), HIV PrEP and post-exposure prophylaxis (PEP), HIV vaccines, and microbicides. Among these potential strategies, PrEP is considered to be one of the most promising strategies in MSM. Several animal and human studies have suggested that ARV drugs might reduce the risk of HIV infection either by PrEP or by non-occupational PEP. A 12-month PrEP clinical trial of daily oral tenofovir disoproxil fumarate (TDF) for HIV prevention was performed among 400 HIV-negative Ghanaian women, and achieved good acceptability and >82% adherence. In November 2010, the US National Institutes of Health (NIH) announced the results of the iPrEx trial of PrEP conducted among 2499 HIV-seronegative MSM in six countries, which showed that daily oral Truvada, a combination of emtricitabine (FTC) and TDF, reduced risk of HIV incidence by 44%, with a median 1.2 years follow-up, compared ...
Physician reviewed emtricitabine, nelfinavir, and tenofovir patient information - includes emtricitabine, nelfinavir, and tenofovir description, dosage and directions.
Tenofovir disoproxil fumarate (TDF) is a prodrug of tenofovir (TFV). That is, TDF is taken orally and converted in the blood stream to TFV that is then converted intracellularly to TFV-diphosphate, which is the pharmacologically-active drug. Abstract 152LB described a new prodrug of TFV-diphosphate, GS-7340, which is more potent and achieves higher intracellular concentrations than does TDF. The in vitro potency as measured by the IC50 for TFV is 1.2 μM, is 0.015 μM for TDF, and is 0.003 μM for GS-7340. TDF (300 mg once daily) and GS-7340 (50 or 150 mg once daily) were given to treatment-naïve, HIV-infected volunteers for 14 days. The time-weighted change in viral load was -0.54 for TDF, -0.95 for 50 mg GS-7340, and -1.07 for 150 mg of GS-7340. Compared with TDF, the plasma concentrations of TFV were approximately 90% lower and the intracellular PBMC concentrations were variable but some 30-fold higher with 150 mg of GS-7340. There was no difference in short-term safety. GS-7340 represents a ...
Five year efficacy and safety of tenofovir-based salvage therapy for patients with chronic hepatitis B who previously failed LAM/ADV therapy ...
TAF is also being studied in a second ongoing Phase 2 trial evaluating a single tablet regimen containing TAF, Janssen R&D Irelands protease inhibitor Prezista® (darunavir), cobicistat and emtricitabine compared to Truvada® (emtricitabine and tenofovir disoproxil fumarate) plus Prezista and cobicistat, dosed as individual components. The study is fully enrolled and 24-week results will be available in the first half of 2013. About the Study The Phase 2 study is a randomized, double-blind 48-week clinical trial among HIV-1 infected adults with HIV RNA levels (viral load) greater than or equal to 5,000 copies/mL and CD4 cell counts greater than 50 cells/mm3. A total of 170 patients were randomized (2:1) to receive a once-daily tablet containing TAF 10 mg/elvitegravir 150 mg/cobicistat 150 mg/emtricitabine 200 mg (n=112) or Stribild (n=58). Bone mineral density was assessed in all patients by DEXA scans at baseline and at week 24. The study is ongoing. Secondary endpoints will include the ...
Crystal structure of PhnZ in complex with substrate reveals a di-iron oxygenase mechanism for catabolism of organophosphonates ... Crystal structure of PhnZ in complex with substrate reveals a di-iron oxygenase mechanism for catabolism of organophosphonates. ... Crystal structure of PhnZ in complex with substrate reveals a di-iron oxygenase mechanism for catabolism of organophosphonates. ...
Methods for the detection of polar organophosphonates like the herbicide glyphosate and its metabolite aminomethylphosphonic ... Analysis of the herbicide glyphosate and related organophosphonates in seawater : overcoming salt-matrix-induced limitations. ... Methods for the detection of polar organophosphonates like the herbicide glyphosate and its metabolite aminomethylphosphonic ...
Carbon-containing phosphonic acid compounds. Included under this heading are compounds that have carbon bound to either OXYGEN atom or the PHOSPHOROUS atom of the (P=O)O2 structure.
Kadirov, B. (2020) "MODIFICATION OF COMPOSITION OF SALINITY INHIBITORS BASED ON ORGANOPHOSPHONATES AND ACRYLIC ACID," Technical ... MODIFICATION OF COMPOSITION OF SALINITY INHIBITORS BASED ON ORGANOPHOSPHONATES AND ACRYLIC ACID ...
Organophosphonates 159. Organophosphorus Compounds 159. Organosulfur Compounds with Other Functional Groups 159 ...
Organophosphonates. *Organophosphorus Compounds. CAS number. 66508-53-0. Drug Targets. Name. Target Sequence. Pharmacological ...
Organophosphonates / administration & dosage * Organophosphonates / pharmacology* * Organophosphonates / therapeutic use * RNA- ...
Organophosphonates. Funderburg NT, Andrade A, Chan ES, et al. "Dynamics of immune reconstitution and activation markers in HIV+ ...
Organophosphonates. Hogan CM, Degruttola V, Sun X, et al. "The setpoint study (ACTG A5217): effect of immediate versus deferred ...
Organophosphonates* * Organophosphorus Compounds / therapeutic use * T-Lymphocytopenia, Idiopathic CD4-Positive / complications ...
0 (Antiviral Agents); 0 (Organophosphonates); 8J337D1HZY (Cytosine); JIL713Q00N (cidofovir). [Em] M s de entrada:. 1801. ...
0 (Lanthanoid Series Elements); 0 (Lewis Acids); 0 (Organophosphonates); 0 (Polymers); 05175J654G (Niobium); 60YU5MIG9W ( ...
Organophosphonates / administration & dosage. Organophosphorus Compounds / administration & dosage. Oxazines / administration ... 0/Anti-Retroviral Agents; 0/Drug Combinations; 0/Organophosphonates; 0/Organophosphorus Compounds; 0/Oxazines; 0/Truvada; 0/ ...
Organophosphonates with One. -. , Two. -. , and Three. -. Dimensional Structures. Sanjit Konar, Jerzy Zon, Andrey V. Prosvirin ...
McGrath, J. W., Ternan, N. G., and Quinn, J. P. (1997). Utilization of organophosphonates by environmental microorganisms. Lett ... Ternan, N. G., McGrath, J. W., McMullan, G., and Quinn, J. P. (1998). Organophosphonates: occurrence, synthesis and ...
Organophosphonates revealed: new insights into the microbial metabolism of ancient molecules.. McGrath JW, Chin JP, Quinn JP. ...
Organophosphonates: A review on environmental relevance, biodegradability and removal in wastewater treatment plants. ...
Analysis of Aminopolycarboxylates and Organophosphonates, p. 87. In Biogeochemistry of Chelating Agents, eds. B. Nowack and J. ...
Organophosphonates as model system for studying electronic transport through monolayers on SiO2/Si surfaces. Appl. Phys. Lett. ...
6. Global Organophosphonates Market Outlook. 6.1. Market Size & Forecast. 6.1.1. By Volume. 7. Global Hydroxycarboxylic Acid ... Figure 18: Global Organophosphonates Market Size, By Volume, 2010-2020F (000 MT). Figure 19: Global Hydroxycarboxylic Acid ... Further, the consumption of organophosphonates is expected to witness lower growth over the forecast period, as compared with ... Segmental Analysis - Aminopolycarboxylic, Organophosphonates and Hydroxycarboxylic acid. *Regional Analysis - Asia-Pacific, ...
1 displays the signal/noise ratios at the DVLs for the organophosphonates in the ESI positive mode and Fig. 2 in the ESI ... 1.4 The detection verification level (DVL) and reporting range for the organophosphonates are listed in Table 1. ... referred to collectively as organophosphonates in this test method) in surface water by direct injection using liquid ... The reporting limit is the concentration of the Level 1 calibration standard as shown in Table 2 for the organophosphonates ...
... organo phosphonates, e.g. dibutyl methanephosphonate, dibutyl trichloromethanephosphonate, dibutyl monochloromethanephosphonate ...
Phosphorus NMR as a tool to study mineralization of organophosphonates-The ability of Spirulina spp. to degrade glyphosate. ...
Organophosphonates/administration & dosage/blood/pharmacokinetics*. *Reverse Transcriptase Inhibitors/administration & dosage/ ... Organophosphonates/administration & dosage/blood/pharmacokinetics*. *Reverse Transcriptase Inhibitors/administration & dosage/ ...
Pre-exposure Prophylaxis Prevents Intravaginal HIV-1 Transmission in Humanized BLT Mice(A) Kaplan-Meier plot of the time course to plasma antigenemia conversion
For organophosphonates, some data in the critically evaluated compilations are not consistent with later, more precise results ... Recently, organophosphonates have been identified as promising reagents for the creation of so-called structurally tailored ... Annual industrial output of organophosphonates is in the thousands of tons. The broad and intensive applications of ... Uses of organophosphonates span applications in flame-resistant polymers, photographic processing, ore flotation ( ...
Fuller, F. D., Gul, S., Chatterjee, R., Sethe Burgie, E., Young, I. D., Lebrette, H., Srinivas, V., Brewster, A. S., Michels-Clark, T., Clinger, J. A., Andi, B., Ibrahim, M., Pastor, E., De Lichtenberg, C., Hussein, R., Pollock, C. J., Zhang, M., Stan, C. A., Kroll, T., Fransson, T. & 36 others, Weninger, C., Kubin, M., Aller, P., Lassalle, L., Bräuer, P., Miller, M. D., Amin, M., Koroidov, S., Roessler, C. G., Allaire, M., Sierra, R. G., Docker, P. T., Glownia, J. M., Nelson, S., Koglin, J. E., Zhu, D., Chollet, M., Song, S., Lemke, H., Liang, M., Sokaras, D., Alonso-Mori, R., Zouni, A., Messinger, J., Bergmann, U., Boal, A. K., Martin Bollinger, J., Krebs, C., Högbom, M., Phillips, G. N., Vierstra, R. D., Sauter, N. K., Orville, A. M., Kern, J., Yachandra, V. K. & Yano, J., Feb 27 2017, In : Nature methods. 14, 4, p. 443-449 7 p.. Research output: Contribution to journal › Article ...
Organophosphates and organophosphonates are organophosphorus compounds, which have activity against acetylcholine esterase (the ...
Some specific chelating agents, for example organophosphonates, sodium gluconates, and APCAs are useful in various household ...
  • Methods for the detection of polar organophosphonates like the herbicide glyphosate and its metabolite aminomethylphosphonic acid (AMPA) in seawater were developed within this thesis. (uni-rostock.de)
  • Organophosphates, organophosphonates (henceforth jointly abbreviated as OP) and carbamates are typical anticholinergic compounds which are widely known as pesticides or nerve agents [ 1 ]. (mdpi.com)
  • Uses of organophosphonates span applications in flame-resistant polymers, photographic processing, ore flotation (aminophosphonic surfactants), actinide separation processes, and analytical chemistry. (iupac.org)
  • Aminopolycarboxylic acid, hydroxycarboxylic acid, and organophosphonates, are the three different classes of chelating agents consumed globally, wherein, the consumption of aminopolycarboxylic acid is the highest. (marketresearch.com)
  • Further, the consumption of organophosphonates is expected to witness lower growth over the forecast period, as compared with aminopolycarboxylic acid and hydroxycarboxylic acid. (marketresearch.com)
  • 1.1 This procedure covers the determination of diisopropyl methylphosphonate (DIMP), ethyl hydrogen dimethylamidophosphate (EHDMAP), ethyl methylphosphonic acid (EMPA), isopropyl methylphosphonic acid (IMPA), methylphosphonic acid (MPA) and pinacolyl methylphosphonic acid (PMPA) (referred to collectively as organophosphonates in this test method) in surface water by direct injection using liquid chromatography (LC) and detected with tandem mass spectrometry (MS/MS) using electrospray ionization (ESI). (bsigroup.com)
  • PM-IRRAS studies of the adsorption and stability of organophosphonates monolayers on passivated NiTi surfaces. (mpie.de)
  • Ermakova IT, Shushkova TV, Leontievsky AA (2008) Microbial degradation of organophosphonates by soil bacteria. (springer.com)
  • The broad and intensive applications of organophosphonates require reliable data on the stability constants of the corresponding complexes in order to permit equilibrium modeling and prediction of the important technological, environmental, and pharmacokinetic equilibria. (iupac.org)
  • Recently, organophosphonates have been identified as promising reagents for the creation of so-called structurally tailored materials and microporous materials, in catalysis, and in the electrochemical treatment of polluted soils. (iupac.org)