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Xenobiotica
the fate of foreign compounds in biological systems
Volume 32, 2002 - Issue 1
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Original Article

CYP3A4-mediated hepatic metabolism of the HIV-1 protease inhibitor saquinavir in vitro

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Pages 1-17 | Received 04 May 2001, Published online: 12 Jul 2010

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Kevin A. Ford, Gregory Ryslik, Jasleen Sodhi, Jason Halladay, Dolo Diaz, Donna Dambach & Melisa Masuda. (2015) Computational predictions of the site of metabolism of cytochrome P450 2D6 substrates: comparative analysis, molecular docking, bioactivation and toxicological implications. Drug Metabolism Reviews 47:3, pages 291-319.
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Sidi Yang, Yufei Chen, Kaien Gu, Alicia Dash, Casey L Sayre, Neal M Davies & Emmanuel A Ho. (2013) Novel intravaginal nanomedicine for the targeted delivery of saquinavir to CD4+ immune cells. International Journal of Nanomedicine 8, pages 2847-2858.
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Kilari Eswar Kumar & Shaik Mastan. (2011) Effect of protease inhibitors (indinavir and ritonavir) on the pharmacokinetics of gliclazide in rabbits. Research and Reports in Endocrine Disorders 1, pages 1-9.
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Mona Arab-Alameddine, Laurent Arhtur Décosterd, Thierry Buclin, Amalio Telenti & Chantal Csajka. (2011) Antiretroviral drug toxicity in relation to pharmacokinetics, metabolic profile and pharmacogenetics. Expert Opinion on Drug Metabolism & Toxicology 7:5, pages 609-622.
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Burcin Yavuz, Jessica L. Morgan, Laura Showalter, Katti R. Horng, Satya Dandekar, Carolina Herrera, Patricia LiWang & David L. Kaplan. (2018) Pharmaceutical Approaches to HIV Treatment and Prevention. Advanced Therapeutics 1:6, pages 1800054.
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Michael A. Collier, Matthew D. Gallovic, Eric M. Bachelder, Craig D. Sykes, Angela Kashuba & Kristy M. Ainslie. (2016) Saquinavir Loaded Acetalated Dextran Microconfetti – a Long Acting Protease Inhibitor Injectable. Pharmaceutical Research 33:8, pages 1998-2009.
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Feng Li, Jie Lu & Xiaochao Ma. (2014) CPY3A4-Mediated α -Hydroxyaldehyde Formation in Saquinavir Metabolism . Drug Metabolism and Disposition 42:2, pages 213-220.
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Zhiying Wang, Dhananjay Pal & Ashim K. Mitra. (2012) Stereoselective Evasion of P-glycoprotein, Cytochrome P450 3A, and Hydrolases by Peptide Prodrug Modification of Saquinavir. Journal of Pharmaceutical Sciences 101:9, pages 3199-3213.
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Veronique Michaud, Tamara Bar-Magen, Jacques Turgeon, David Flockhart, Zeruesenay Desta & Mark A. Wainberg. (2012) The Dual Role of Pharmacogenetics in HIV Treatment: Mutations and Polymorphisms Regulating Antiretroviral Drug Resistance and Disposition. Pharmacological Reviews 64:3, pages 803-833.
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Carolina Horta Andrade, Lenis Medeiros de Freitas & Valéria de Oliveira. (2011) Twenty-six years of HIV science: an overview of anti-HIV drugs metabolism. Brazilian Journal of Pharmaceutical Sciences 47:2, pages 209-230.
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R. Lledó-García, A. Nácher, V. G. Casabó & M. Merino-Sanjuán. (2011) A Pharmacokinetic Model for Evaluating the Impact of Hepatic and Intestinal First-Pass Loss of Saquinavir in the Rat. Drug Metabolism and Disposition 39:2, pages 294-301.
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Jianghong Fan, Han‐Joo Maeng & K. Sandy Pang. (2010) Interplay of transporters and enzymes in the Caco‐2 cell monolayer: I. effect of altered apical secretion. Biopharmaceutics & Drug Disposition 31:4, pages 215-227.
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Shayne Cox GadEugene G. Hrycay & Stelvio M. Bandiera. 2010. Pharmaceutical Sciences Encyclopedia. Pharmaceutical Sciences Encyclopedia.
Tai Ning Lam & C. Anthony Hunt. (2010) Mechanistic Insight from In Silico Pharmacokinetic Experiments: Roles of P-glycoprotein, Cyp3A4 Enzymes, and Microenvironments. Journal of Pharmacology and Experimental Therapeutics 332:2, pages 398-412.
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Akihiro Hisaka, Yoshiyuki Ohno, Takehito Yamamoto & Hiroshi Suzuki. (2010) Prediction of pharmacokinetic drug–drug interaction caused by changes in cytochrome P450 activity using in vivo information. Pharmacology & Therapeutics 125:2, pages 230-248.
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N. Treijtel, J.C.H. van Eijkeren, S. Nijmeijer, I.C.J. de Greef-van der Sandt & A.P. Freidig. (2009) Clearance and clearance inhibition of the HIV-1 protease inhibitors ritonavir and saquinavir in sandwich-cultured rat hepatocytes and rat microsomes. Toxicology in Vitro 23:1, pages 185-193.
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Tai Ning Lam & C. Anthony Hunt. (2008) Mechanistic simulations explain paradoxical saquinavir metabolism during in vitro vectorial transport study. Mechanistic simulations explain paradoxical saquinavir metabolism during in vitro vectorial transport study.
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Helen H. Usansky, Peidi Hu & Patrick J. Sinko. (2008) Differential Roles of P-Glycoprotein, Multidrug Resistance-Associated Protein 2, and CYP3A on Saquinavir Oral Absorption in Sprague-Dawley Rats. Drug Metabolism and Disposition 36:5, pages 863-869.
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Stéphane J. Mouly, Mary F. Paine & Paul B. Watkins. (2004) Contributions of CYP3A4, P-glycoprotein, and Serum Protein Binding to the Intestinal First-Pass Extraction of Saquinavir. Journal of Pharmacology and Experimental Therapeutics 308:3, pages 941-948.
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Gerd Mikus, Laila Schmidt, J??rgen Burhenne, Reinhard Ding, Klaus-Dieter Riedel, Yorki Tayrouz, Johanna Weiss & Walter Emil Haefeli. (2004) Reduction of Saquinavir Exposure by Coadministration of Loperamide. Clinical Pharmacokinetics 43:14, pages 1015-1024.
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