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Kelen C C Soares et al.
Journal of pharmaceutical sciences, 102(8), 2409-2423 (2013-06-12)
Literature data on the properties of zidovudine relevant to waiver of in vivo bioequivalence (BE) testing requirements for the approval of immediate-release (IR) solid oral dosage forms containing zidovudine alone or in combination with other active pharmaceutical ingredients (APIs) are
Youko Suehiro et al.
British journal of haematology, 169(3), 356-367 (2015-01-24)
Adult T cell leukaemia/lymphoma (ATL) is a human T cell leukaemia virus type-I (HTLV-I)-infected T cell malignancy with poor prognosis. We herein developed a novel therapeutic vaccine designed to augment an HTLV-I Tax-specific cytotoxic T lymphocyte (CTL) response that has
Cátia Teixeira et al.
European journal of medicinal chemistry, 46(4), 979-992 (2011-02-25)
The first anti-HIV drug, zidovudine (AZT), was approved by the FDA a quarter of a century ago, in 1985. Currently, anti-HIV drug-combination therapies only target HIV-1 protease and reverse transcriptase. Unfortunately, most of these molecules present numerous shortcomings such as
J Darbyshire et al.
The Cochrane database of systematic reviews, (3)(3), CD002039-CD002039 (2000-07-25)
Zidovudine (AZT) monotherapy was the first antiretroviral drug to be tested widely. Subsequent trials in asymptomatic or early symptomatic HIV infection indicated short-term delays in disease progression with AZT, but not improved survival. To assess the effects of immediate versus
J Darbyshire et al.
The Cochrane database of systematic reviews, (3)(3), CD002038-CD002038 (2000-07-25)
Zidovudine (AZT) monotherapy was the first antiretroviral drug to be tested widely. The next two drugs to be developed were didanosine (ddI) and zalcitabine (ddC). To assess the effects of zidovudine (AZT), zidovudine plus didanosine (ddI) and zidovudine plus zalcitabine
J Darbyshire et al.
The Cochrane database of systematic reviews, (2)(2), CD002039-CD002039 (2000-05-05)
Zidovudine (AZT) monotherapy was the first antiretroviral drug to be tested widely. Subsequent trials in asymptomatic or early symptomatic HIV infection indicated short-term delays in disease progression with AZT, but not improved survival. To assess the effects of immediate versus
Rima Kulkarni et al.
Antimicrobial agents and chemotherapy, 58(10), 6145-6150 (2014-08-06)
Highly active antiretroviral therapy (HAART) involves combination treatment with three or more antiretroviral agents. The antiviral effects of combinations of emtricitabine (FTC) plus tenofovir (TFV) plus antiretroviral agents of all the major drug classes were investigated. Combinations of FTC and
Shilin Cheung et al.
Journal of pharmaceutical and biomedical analysis, 94, 12-18 (2014-02-19)
CE coupled with UV detection was assessed as a possible platform for the chemical identity and purity analysis of positron emission tomography (PET) tracers using [(18)F]FAC and [(18)F]FLT as examples. Representative samples containing mixtures of the tracers plus well-known impurities
Alicen Spaulding et al.
The Cochrane database of systematic reviews, (8)(8), CD008651-CD008651 (2010-08-06)
The introduction of highly active antiretroviral therapy (ART) as treatment for HIV infection has greatly improved mortality and morbidity for adults and children living with HIV around the world. Two common medications given in first-line antiretroviral therapy are the nucleoside
Martin Stürmer et al.
Antiviral therapy, 12(5), 695-703 (2007-08-24)
Highly active antiretroviral therapy (HAART) has significantly reduced morbidity and mortality in HIV-infected patients. However, problems such as short-term or long-term toxicity and the development of drug resistance could necessitate a change in the therapy regimen. Whereas various HAART options
Andrew Rowland et al.
Drug metabolism and disposition: the biological fate of chemicals, 43(1), 147-153 (2014-11-09)
This study characterized the kinetics, variability, and factors that affect UDP-glucuronic acid (UDP-GlcUA) uptake by human liver microsomes (HLM). Biphasic kinetics were observed for UDP-GlcUA uptake by HLM. Uptake affinities (assessed as Kd) of the high- and low-affinity components differed
Kyra J Barnes et al.
European journal of clinical pharmacology, 70(9), 1097-1106 (2014-06-24)
To investigate the potential inhibitory effects of uremic toxins on the major human hepatic drug-metabolising cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzymes in vitro. Benzyl alcohol, p-cresol, indoxyl sulfate, hippuric acid and a combination of the four uremic toxins were
Guillaume Margaillan et al.
Drug metabolism and disposition: the biological fate of chemicals, 43(4), 611-619 (2015-02-05)
Renal metabolism by UDP-glucuronosyltransferase (UGT) enzymes is central to the clearance of many drugs. However, significant discrepancies about the relative abundance and activity of individual UGT enzymes in the normal kidney prevail among reports, whereas glucuronidation in tumoral kidney has
Y-H Lai et al.
Gene therapy, 22(2), 155-162 (2014-10-31)
Replicating virus vectors are attractive tools for anticancer gene therapy, but the potential for adverse events due to uncontrolled spread of the vectors has been a major concern. To design a tumor-specific retroviral replicating vector (RRV), we replaced the U3
Tomas Cihlar et al.
Antiviral research, 85(1), 39-58 (2009-11-06)
Twenty-five years ago, nucleoside analog 3'-azidothymidine (AZT) was shown to efficiently block the replication of HIV in cell culture. Subsequent studies demonstrated that AZT acts via the selective inhibition of HIV reverse transcriptase (RT) by its triphosphate metabolite. These discoveries
Soo Hyeon Bae et al.
Antimicrobial agents and chemotherapy, 58(9), 5036-5046 (2014-06-04)
Macrolactin A (MA) and 7-O-succinyl macrolactin A (SMA), polyene macrolides containing a 24-membered lactone ring, show antibiotic effects superior to those of teicoplanin against vancomycin-resistant enterococci and methicillin-resistant Staphylococcus aureus. MA and SMA are currently being evaluated as antitumor agents
Zhufeng Wu et al.
The Journal of pharmacy and pharmacology, 67(4), 583-596 (2014-12-17)
To determine the reaction kinetics for regioselective glucuronidation of gingerols (i.e. 6-, 8- and 10-gingerol) by human liver microsomes and expressed UDP-glucuronosyltransferase (UGT) enzymes, and to identify the main UGT enzymes involved in regioselective glucuronidation of gingerols. The rates of
Tim Ibbotson et al.
Drugs, 63(11), 1089-1098 (2003-05-17)
The triple combination tablet containing lamivudine (150 mg), zidovudine (300 mg) and abacavir (300 mg, as abacavir sulfate) is a new formulation of three nucleoside analogue reverse transcriptase inhibitors. Two studies in treatment-naive patients (one double-blind, one nonblind) have reported
G Skowron et al.
The American journal of medicine, 88(5B), 20S-23S (1990-05-21)
The deoxynucleoside analogues 2',3'-dideoxy-cytidine (ddC) and 3'-azido-3'-deoxythymidine (zidovudine, AZT) are active as single agents in conferring immunologic and virologic benefits in patients with acquired immunodeficiency syndrome (AIDS) or AIDS-related complex. Both drugs, however, produce dose-limiting toxicities. AZT is associated with
R Bendayan et al.
Pharmacotherapy, 15(3), 338-344 (1995-05-01)
In humans and various animal species, 3'-azido-3'-deoxythymidine (AZT) is in part eliminated by the kidneys, where it undergoes significant tubular secretion. The goal of this project was to develop, in a continuous renal epithelial cell line (LLCPK1), a model of
Mike De Vrieze et al.
Analytical and bioanalytical chemistry, 406(25), 6179-6188 (2014-08-16)
Over the past decades, several in vitro methods have been tested for their ability to predict drug penetration across the blood-brain barrier. So far, in high-performance liquid chromatography, most attention has been paid to micellar liquid chromatography and immobilized artificial
Alicen Spaulding et al.
The Cochrane database of systematic reviews, (10)(10), CD008740-CD008740 (2010-10-12)
The introduction of highly active antiretroviral therapy (ART) as treatment for HIV infection has greatly improved mortality and morbidity for adults and children living with HIV around the world. Two of the most common medications given in first-line ART are
Deidra D Parrish et al.
International journal of STD & AIDS, 25(5), 355-359 (2013-10-10)
We conducted a study to assess trends in haemoglobin recovery among HIV-infected patients initiated on zidovudine-based combination antiretroviral therapy (cART) stratified by baseline haemoglobin level. Haemoglobin data from non-pregnant adult patients initiating cART in rural north-central Nigeria between June 2009
A fossil record of zidovudine resistance in transmitted isolates of HIV-1.
D R Kuritzkes
Proceedings of the National Academy of Sciences of the United States of America, 98(24), 13485-13487 (2001-11-22)
Seung Jun Lee et al.
Toxicology letters, 232(2), 458-465 (2014-12-03)
In the present study, we evaluated the inhibitory potentials of finasteride for the major human hepatic UDP-glucuronosyltransferases (UGTs) (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, UGT2B7, and UGT2B15) in vitro using LC-MS/MS by specific marker reactions in human liver microsomes (except for
Ester Ballana et al.
Antimicrobial agents and chemotherapy, 58(8), 4804-4813 (2014-06-11)
Sterile alpha motif and histidine-aspartic domain-containing protein 1 (SAMHD1) is a deoxynucleoside triphosphate (dNTP) triphosphohydrolase recently recognized as an antiviral factor that acts by depleting dNTP availability for viral reverse transcriptase (RT). SAMHD1 restriction is counteracted by the human immunodeficiency
Hua Sun et al.
Journal of pharmaceutical sciences, 104(1), 244-256 (2014-11-14)
In this study, we aimed to determine the modulatory effects of warfarin (an extensively used anticoagulant drug) and its metabolites on UDP-glucuronosyltransferase (UGT) activity and to assess the potential of warfarin to alter the pharmacokinetics of zidovudine (AZT). The effects
Yu Fen Zheng et al.
Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association, 68, 117-127 (2014-03-19)
We evaluated the potential of BST204, a purified dry extract of ginseng, to inhibit or induce human liver cytochrome P450 enzymes (CYPs) and UDP-glucuronosyltransferases (UGTs) in vitro to assess its safety. In vitro drug interactions of four bioactive ginsenosides of
Muki S Shey et al.
The Cochrane database of systematic reviews, 3(3), CD005481-CD005481 (2013-04-02)
UNAIDS estimates that 34 million people are currently living with the human immunodeficiency virus (HIV) worldwide. Currently recommended regimens for initiating HIV treatment consist of either a non-nucleoside reverse transcriptase inhibitor (NNRTI) or ritonavir-boosted protease inhibitor (PI) combined with two
H G Sprenger et al.
HIV medicine, 16(2), 122-131 (2014-12-05)
The aim of the study was to test the antiviral efficacy of a triple nucleoside reverse transcriptase inhibitor (NRTI) regimen, with potential beneficial metabolic effects, as maintenance therapy after induction with dual NRTIs and a boosted protease inhibitor (PI). An
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