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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...
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...
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...
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), 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...
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...
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...
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...
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...
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...
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...
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...
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...
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...
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)
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...
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...
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...
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...
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...
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...
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...
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...
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...
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...
W Mattes et al.
Toxicology letters, 230(3), 467-478 (2014-08-03)
While conventional parameters used to detect hepatotoxicity in drug safety assessment studies are generally informative, the need remains for parameters that can detect the potential for hepatotoxicity at lower doses and/or at earlier time points. Previous work has shown that...
C Foster et al.
HIV medicine, 10(7), 397-406 (2009-05-23)
Zidovudine (ZDV) has been the cornerstone of antiretroviral (ARV) therapy for pregnant women infected with HIV-1 in the prevention of mother-to-child transmission (MTCT) and remains the only licensed ARV for use in pregnancy. We explored the current and future roles...
Eriko Higashi et al.
Biopharmaceutics & drug disposition, 35(6), 313-320 (2014-04-23)
The microminipig, a small minipig, was bred as a novel experimental animal for nonclinical pharmacology/toxicology studies by Fuji Micra Inc. (Shizuoka, Japan). Species differences in drug metabolism between humans and the microminipig need to be elucidated in more detail in...
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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