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J Mol Model 2010,Oct,01;16(10):1577-83; (PMID: 20195662) [...]In the present work we investigated the structural properties of a triple mutant (I54V-V82A-L90M) and a double mutant (V82A-L90M) that both confer strong resistance to ritonavir (RTV), but not to amprenavir (APV). For the unliganded double mutant protease molecular dynamics simulations revealed a contraction of the [...]
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J Pharm Biomed Anal 2010,Sep,05;52(5):774-80; (PMID: 20236784) [...]A bioanalytical method for the determination of most commonly prescribed protease inhibitors (saquinavir, atazanavir, amprenavir, darunavir, lopinavir and ritonavir) and non-nucleoside reverse transcriptase inhibitors (etravirine, [...]
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Drug Metab Dispos 2010,Aug,01;38(8):1355-61; (PMID: 20427691) [...]The tool compounds are lipophilic transcellular drugs [GlaxoSmithKline (GSK)-A, GSK-B, GSK-C, and naproxen], lipophilic P-glycoprotein (P-gp) substrates (amprenavir and loperamide), and hydrophilic paracellular compounds (sodium fluorescein and atenolol). Our data showed that rate and extent of CNS penetration for lipophilic transcellular drugs and [...]
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Clin Chem Lab Med 2010,Aug,01;48(8):1153-5; (PMID: 20482447) [...]BACKGROUND: We previously developed a method for the simultaneous determination of the human immunodeficiency protease inhibitors: amprenavir, atazanavir, darunavir, indinavir, lopinavir, nelfinavir, ritonavir, saquinavir and [...]
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Arch Intern Med 2010,Jul,26;170(14):1228-38; (PMID: 20660842) [...]Cumulative exposure to all PIs except saquinavir was associated with an increased risk of MI significant for amprenavir/fosamprenavir with or without ritonavir (OR, 1.53; 95% CI, 1.21-1.94 per year) and lopinavir[...]
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Biopharm Drug Dispos 2010,Jul,01;31(5-6):278-85; (PMID: 20578213) [...] with compounds that exhibit strong subject-dependent permeability. This was demonstrated by identifying an interaction between amprenavir and ketoconazole (P-gp and CYP3A inhibitor) in five out of seven rats (permeability increase between 1.9- and 4.2-fold), despite high inter-individual differences in intrinsic permeability for [...]
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J Chromatogr B Analyt Technol Biomed Life Sci 2010,Jun,01;878(19):1455-65; (PMID: 20427248) [...]Here we describe a simple, fast and sensitive HPLC-MS/MS method for determination of the commonly used protease inhibitors (PI) amprenavir, atazanavir, darunavir, lopinavir, ritonavir, saquinavir and the non-nucleoside reverse transcriptase inhibitor (NNRTI) [...]
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Anal Bioanal Chem 2010,May,01;397(1):189-203; (PMID: 19998025) Fosamprenavir is a pro-drug of the antiretroviral protease inhibitor amprenavir and is oxidizable at solid electrodes. The anodic oxidation behavior of fosamprenavir was investigated using cyclic and linear sweep voltammetry at boron-doped diamond and glassy [...]
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HIV Med 2010,Mar,01;11(3):193-9; (PMID: 19863619) [...]Twenty-four-hour pharmacokinetic sampling was carried out on day 7 of period 1 and on day 14 of periods 2 and 3. Steady-state plasma amprenavir (APV) and tenofovir (TFV) pharmacokinetics were assessed by noncompartmental analysis and parameter values observed with each regimen were compared using geometric mean ratios with 90% confidence intervals.[...]
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FEMS Yeast Res 2010,Mar,01;10(2):221-4; (PMID: 20030734) [...] that participate in multiple aspects of the fungal biology and pathogenesis. In the present paper, we have shown that amprenavir, a peptidase inhibitor used in HIV chemotherapy, inhibited Sap2 and growth of C. albicans and also promoted ultrastructural alterations.[...]
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