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Xenobiotica
the fate of foreign compounds in biological systems
Volume 42, 2012 - Issue 2
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Clinical Pharmacokinetics and Metabolism

Cross-species absorption, metabolism, distribution and pharmacokinetics of BI 201335, a potent HCV genotype 1 NS3/4A protease inhibitor

Jianmin DuanDepartment of Biological Sciences, Research and development, Boehringer Ingelheim Canada Ltd., Laval, Quebec, CanadaCorrespondence[email protected]
,
Chan-Loi YongDepartment of Clinical Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, USA
,
Michel GarneauDepartment of Biological Sciences, Research and development, Boehringer Ingelheim Canada Ltd., Laval, Quebec, Canada
,
Ma’an AmadDepartment of Biological Sciences, Research and development, Boehringer Ingelheim Canada Ltd., Laval, Quebec, Canada
,
Gordon BolgerDepartment of Biological Sciences, Research and development, Boehringer Ingelheim Canada Ltd., Laval, Quebec, Canada
,
Josie De MarteDepartment of Biological Sciences, Research and development, Boehringer Ingelheim Canada Ltd., Laval, Quebec, Canada
,
Hélène MontpetitDepartment of Biological Sciences, Research and development, Boehringer Ingelheim Canada Ltd., Laval, Quebec, Canada
,
Francois OtisDepartment of Biological Sciences, Research and development, Boehringer Ingelheim Canada Ltd., Laval, Quebec, Canada
,
Martin JutrasDepartment of Biological Sciences, Research and development, Boehringer Ingelheim Canada Ltd., Laval, Quebec, Canada
,
Manon RhéaumeDepartment of Biological Sciences, Research and development, Boehringer Ingelheim Canada Ltd., Laval, Quebec, Canada
,
Peter W. WhiteDepartment of Biological Sciences, Research and development, Boehringer Ingelheim Canada Ltd., Laval, Quebec, Canada
,
Montse Llinàs-BrunetDepartment of Medicinal Chemistry, Research and development, Boehringer Ingelheim Canada Ltd., Laval, Quebec, Canada
,
Richard C. BethellDepartment of Biological Sciences, Research and development, Boehringer Ingelheim Canada Ltd., Laval, Quebec, Canada
&
Michael G. CordingleyScientific Administration, Research and development, Boehringer Ingelheim Canada Ltd., Quebec, Canada
 show all
Pages 164-172 | Received 07 Jul 2011, Accepted 04 Aug 2011, Published online: 11 Oct 2011

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Natalia Lorna Laufer & Jürgen Kurt Rockstroh. (2014) Faldaprevir (BI 201335) for the treatment of hepatitis C in patients co-infected with HIV. Expert Review of Anti-infective Therapy 12:2, pages 157-164.
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Nathalie Rioux, Joëlle Batonga, Federico Colombo, Jonathan Massé, Christine Zouki, Maria D. Ribadeneira, Jianmin Duan & Richard C. Bethell. (2013) A simplified approach to predict CYP3A-mediated drug–drug interactions at early drug discovery: validation with clinical data. Xenobiotica 43:7, pages 592-597.
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Articles from other publishers (11)

J. Matthew Hutzler, Barbara J. Ring & Shelby R. Anderson. (2015) Low-Turnover Drug Molecules: A Current Challenge for Drug Metabolism Scientists. Drug Metabolism and Disposition 43:12, pages 1917-1928.
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Pierre L. Beaulieu, Gordon Bolger, Dan Deon, Martin Duplessis, Gulrez Fazal, Alexandre Gagnon, Michel Garneau, Steven LaPlante, Timothy Stammers, George Kukolj & Jianmin Duan. (2015) Multi-parameter optimization of aza-follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 2: Impact of lipophilicity on promiscuity and in vivo toxicity. Bioorganic & Medicinal Chemistry Letters 25:5, pages 1140-1145.
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Pierre L. Beaulieu, Gordon Bolger, Martin Duplessis, Alexandre Gagnon, Michel Garneau, Timothy Stammers, George Kukolj & Jianmin Duan. (2015) Aza follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 1: Mitigating the genotoxic liability of an aniline metabolite. Bioorganic & Medicinal Chemistry Letters 25:5, pages 1135-1139.
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Pierre L. Beaulieu, Paul C. Anderson, Richard Bethell, Michael Bös, Yves Bousquet, Christian Brochu, Michael G. Cordingley, Gulrez Fazal, Michel Garneau, James R. Gillard, Stephen Kawai, Martin Marquis, Ginette McKercher, Marc-André Poupart, Timothy Stammers, Bounkham Thavonekham, Dominik Wernic, Jianmin Duan & George Kukolj. (2014) Discovery of BI 207524, an Indole Diamide NS5B Thumb Pocket 1 Inhibitor with Improved Potency for the Potential Treatment of Chronic Hepatitis C Virus Infection. Journal of Medicinal Chemistry 57:23, pages 10130-10143.
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Bradley Croy Doak, Bjӧrn Over, Fabrizio Giordanetto & Jan Kihlberg. (2014) Oral Druggable Space beyond the Rule of 5: Insights from Drugs and Clinical Candidates. Chemistry & Biology 21:9, pages 1115-1142.
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Muhammad Imran, Sobia Manzoor, Nasir Mahmood Khattak, Madiha Khalid, Qazi Laeeque Ahmed, Fahed Parvaiz, Muqddas Tariq, Javed Ashraf, Waseem Ashraf, Sikandar Azam & Muhammad Ashraf. (2013) Current and future therapies for hepatitis C virus infection: from viral proteins to host targets. Archives of Virology 159:5, pages 831-846.
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Benoît Moreau, Jeff A. O’Meara, Josée Bordeleau, Michel Garneau, Cedrickx Godbout, Vida Gorys, Mélissa Leblanc, Elisia Villemure, Peter W. White & Montse Llinàs-Brunet. (2013) Discovery of Hepatitis C Virus NS3-4A Protease Inhibitors with Improved Barrier to Resistance and Favorable Liver Distribution. Journal of Medicinal Chemistry 57:5, pages 1770-1776.
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Diane Ramsden, Donald J. Tweedie, Roger St. George, Lin-Zhi Chen & Yongmei Li. (2014) Generating an In Vitro–In Vivo Correlation for Metabolism and Liver Enrichment of a Hepatitis C Virus Drug, Faldaprevir, Using a Rat Hepatocyte Model (HepatoPac). Drug Metabolism and Disposition 42:3, pages 407-414.
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Diane Ramsden, Donald J. Tweedie, Tom S. Chan, Mitchell E. Taub & Yongmei Li. (2014) Bridging In Vitro and In Vivo Metabolism and Transport of Faldaprevir in Human Using a Novel Cocultured Human Hepatocyte System, HepatoPac. Drug Metabolism and Disposition 42:3, pages 394-406.
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Yongmei Li, Jin Zhou, Diane Ramsden, Mitchell E. Taub, Drané O'Brien, Jun Xu, Carl A. Busacca, Nina Gonnella & Donald J. Tweedie. (2014) Enzyme-Transporter Interplay in the Formation and Clearance of Abundant Metabolites of Faldaprevir Found in Excreta but not in Circulation. Drug Metabolism and Disposition 42:3, pages 384-393.
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Jianmin Duan, Gordon Bolger, Michel Garneau, Ma'an Amad, Joëlle Batonga, Hélène Montpetit, François Otis, Martin Jutras, Nicole Lapeyre, Manon Rhéaume, George Kukolj, Peter W. White, Richard C. Bethell & Michael G. Cordingley. (2012) The Liver Partition Coefficient-Corrected Inhibitory Quotient and the Pharmacokinetic-Pharmacodynamic Relationship of Directly Acting Anti-Hepatitis C Virus Agents in Humans. Antimicrobial Agents and Chemotherapy 56:10, pages 5381-5386.
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