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Xenobiotica
the fate of foreign compounds in biological systems
Volume 27, 1997 - Issue 6
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Research Article

Metabolism of the calcium antagonist, mibefradil (POSICORTM, Ro 40-5967). Part III. Comparative pharmacokinetics of mibefradil and its major metabolites in rat, marmoset, cynomolgus monkey and man

H. R. WILTSHIRE Department of Pharmacokinetics and Metabolism, Roche Products Ltd, 40 Broadwater Road, Welwyn Garden City AL7 3AY, UK F. Homann-La Roche AG, Postfach, Basel, CH-4002, Switzerland
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B. M. SUTTON Department of Pharmacokinetics and Metabolism, Roche Products Ltd, 40 Broadwater Road, Welwyn Garden City AL7 3AY, UK F. Homann-La Roche AG, Postfach, Basel, CH-4002, Switzerland
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G. HEEPS Department of Pharmacokinetics and Metabolism, Roche Products Ltd, 40 Broadwater Road, Welwyn Garden City AL7 3AY, UK F. Homann-La Roche AG, Postfach, Basel, CH-4002, Switzerland
,
A. M. BETTY Department of Pharmacokinetics and Metabolism, Roche Products Ltd, 40 Broadwater Road, Welwyn Garden City AL7 3AY, UK F. Homann-La Roche AG, Postfach, Basel, CH-4002, Switzerland
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D. W. ANGUS Department of Pharmacokinetics and Metabolism, Roche Products Ltd, 40 Broadwater Road, Welwyn Garden City AL7 3AY, UK F. Homann-La Roche AG, Postfach, Basel, CH-4002, Switzerland
,
S. R. HARRIS Department of Pharmacokinetics and Metabolism, Roche Products Ltd, 40 Broadwater Road, Welwyn Garden City AL7 3AY, UK F. Homann-La Roche AG, Postfach, Basel, CH-4002, Switzerland
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E. WORTH Department of Pharmacokinetics and Metabolism, Roche Products Ltd, 40 Broadwater Road, Welwyn Garden City AL7 3AY, UK F. Homann-La Roche AG, Postfach, Basel, CH-4002, Switzerland
&
H. A. WELKER Department of Pharmacokinetics and Metabolism, Roche Products Ltd, 40 Broadwater Road, Welwyn Garden City AL7 3AY, UK F. Homann-La Roche AG, Postfach, Basel, CH-4002, Switzerland
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Pages 557-571 | Published online: 22 Sep 2008

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Shogo Matsumoto, Shotaro Uehara, Hidetaka Kamimura, Hiroshi Ikeda, Satoshi Maeda, Machiko Hattori, Megumi Nishiwaki, Kazuhiko Kato & Hiroshi Yamazaki. (2021) Human total clearance values and volumes of distribution of typical human cytochrome P450 2C9/19 substrates predicted by single-species allometric scaling using pharmacokinetic data sets from common marmosets genotyped for P450 2C19. Xenobiotica 51:4, pages 479-493.
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N. Sekiguchi, M. Kato, M. Takada, H. Watanabe, A. Higashida, S. Sakai, M. Ishigai & Y. Aso. (2008) approach for the evaluation of mechanism-based inhibition of cytochrome P450 3A in rats. Xenobiotica 38:4, pages 368-381.
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R. J. WEAVER, M. DICKINS & M. D. BURKE. (1999) A comparison of basal and induced hepatic microsomal cytochrome P450 monooxygenase activities in the cynomolgus monkey (Macaca fascicularis) and man. Xenobiotica 29:5, pages 467-482.
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H. R. WILTSHIRE*B. M. SUTTON, G. HEEPS, A. M. BETTY, D. W. ANGUS, M. J. MADIGAN & S. R. SHARP. (1997) Metabolism of the calcium antagonist, mibefradil (POSICOR™, Ro 40-5967). Part II. Metabolism in hepatic microsomes from rat, marmoset, cynomolgus monkey, rabbit and man. Xenobiotica 27:6, pages 539-556.
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Articles from other publishers (16)

Guilherme H. Souza Bomfim, Erna Mitaishvili, Talita Ferreira Aguiar & Rodrigo S. Lacruz. (2021) Mibefradil alters intracellular calcium concentration by activation of phospholipase C and IP3 receptor function. Molecular Biomedicine 2:1.
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Saganuwan Alhaji Saganuwan. (2021) Application of modified Michaelis – Menten equations for determination of enzyme inducing and inhibiting drugs. BMC Pharmacology and Toxicology 22:1.
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Yong-Wook Son, Ha-Ni Choi, Jeong-Hwan Che, Byeong-Cheol Kang & Jun-Won Yun. (2020) Advances in selecting appropriate non-rodent species for regulatory toxicology research: Policy, ethical, and experimental considerations. Regulatory Toxicology and Pharmacology 116, pages 104757.
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Christopher R. Wellaway, Dominique AmansPaul Bamborough, Heather BarnettRino A. BitJack A. BrownNeil R. Carlson, Chun-wa ChungAnthony W. J. CooperPeter D. CraggsRobert P. DavisTony W. DeanJohn P. EvansLaurie GordonIsobel L. HaradaDavid J. Hirst, Philip G. Humphreys, Katherine L. JonesAntonia J. LewisMatthew J. LindonDave LugoMahnoor MahmoodScott McClearyPatricia Medeiros, Darren J. MitchellMichael O’SullivanArmelle Le GallVipulkumar K. PatelChris PattenDarren L. PooleRishi R. Shah, Jane E. SmithKayleigh A. J. StaffordPamela J. ThomasMythily VimalIan D. WallRobert J. WatsonNatalie WellawayGang Yao & Rab K. Prinjha. (2020) Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening. Journal of Medicinal Chemistry 63:2, pages 714-746.
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Arisa Higa, Hirotaka Hoshi, Yuka Yanagisawa, Emi Ito, Gaku Morisawa, Jun-ichi Imai, Shinya Watanabe & Motoki Takagi. (2017) Evaluation system for arrhythmogenic potential of drugs using human-induced pluripotent stem cell-derived cardiomyocytes and gene expression analysis. The Journal of Toxicological Sciences 42:6, pages 755-761.
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Panos Macheras & Athanassios IliadisPanos Macheras & Athanassios Iliadis. 2016. Modeling in Biopharmaceutics, Pharmacokinetics and Pharmacodynamics. Modeling in Biopharmaceutics, Pharmacokinetics and Pharmacodynamics 161 189 .
Ji Eun Lee, Tae Hui Kwon, Su Jin Gu, Duck-Hyung Lee, B. Moon Kim, Jae Yeol Lee, Jae Kyun Lee, Seon Hee Seo, Ae Nim Pae, Gyochang Keum, Yong Seo Cho & Sun-Joon Min. (2014) Efficient synthesis of mibefradil analogues: an insight into in vitro stability. Organic & Biomolecular Chemistry 12:30, pages 5669.
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Robert S. Foti, Dan A. Rock, Josh T. Pearson, Jan L. Wahlstrom & Larry C. Wienkers. (2011) Mechanism-Based Inactivation of Cytochrome P450 3A4 by Mibefradil through Heme Destruction. Drug Metabolism and Disposition 39:7, pages 1188-1195.
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Nobuo Sekiguchi, Motohiro Kato, Maiko Takada, Hiroo Watanabe, Shotaro Takata, Tetsuya Mitsui, Yoshinori Aso & Masaki Ishigai. (2011) Quantitative Prediction of Mechanism-Based Inhibition Caused by Mibefradil in Rats. Drug Metabolism and Disposition 39:7, pages 1255-1262.
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Peter H. Bui, Arnulfo Quesada, Adrian Handforth & Oliver Hankinson. (2008) The Mibefradil Derivative NNC55-0396, a Specific T-Type Calcium Channel Antagonist, Exhibits Less CYP3A4 Inhibition than Mibefradil. Drug Metabolism and Disposition 36:7, pages 1291-1299.
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Amber S. Tippens. 2007. xPharm: The Comprehensive Pharmacology Reference. xPharm: The Comprehensive Pharmacology Reference 1 5 .
Delphine Jouin, Nadège Blanchard, Eliane Alexandre, Frédéric Delobel, Pascale David-Pierson, Thierry Lavé, Daniel Jaeck, Lysiane Richert & Philippe Coassolo. (2006) Cryopreserved human hepatocytes in suspension are a convenient high throughput tool for the prediction of metabolic clearance. European Journal of Pharmaceutics and Biopharmaceutics 63:3, pages 347-355.
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Gondi N. Kumar, Christopher Sproul, Leszek Poppe, Sharon Turner, Mark Gohdes, Hesham Ghoborah, Desmond Padhi & Lorin Roskos. (2004) METABOLISM AND DISPOSITION OF CALCIMIMETIC AGENT CINACALCET HCL IN HUMANS AND ANIMAL MODELS. Drug Metabolism and Disposition 32:12, pages 1491-1500.
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Hiroyuki Hichiya, Shino Kuramoto, Shigeo Yamamoto, Sumio Shinoda, Nobumitsu Hanioka, Shizuo Narimatsu, Kazuo Asaoka, Atsuro Miyata, Shinichi Iwata, Masahiro Nomoto, Tetsuo Satoh, Kimio Kiryu, Nobuhiko Ueda, Shinsaku Naito, Geoffrey T. Tucker & S.Wynne Ellis. (2004) Cloning and functional expression of a novel marmoset cytochrome P450 2D enzyme, CYP2D30: comparison with the known marmoset CYP2D19. Biochemical Pharmacology 68:1, pages 165-175.
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J. Fuite, R. Marsh & J. Tuszyński. (2002) Fractal pharmacokinetics of the drug mibefradil in the liver. Physical Review E 66:2.
Crossref
Thomayant Prueksaritanont, Bennett Ma, Cuyue Tang, Yuan Meng, Carol Assang, Ping Lu, Paul J. Reider, Jiunn H. Lin & Thomas A. Baillie. (2001) Metabolic interactions between mibefradil and HMG‐CoA reductase inhibitors: an in vitro investigation with human liver preparations . British Journal of Clinical Pharmacology 47:3, pages 291-298.
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