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Xenobiotica
the fate of foreign compounds in biological systems
Volume 35, 2005 - Issue 6
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Research Article

Microsomal prediction of in vivo clearance and associated interindividual variability of six benzodiazepines in humans

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Pages 603-625 | Received 14 Mar 2005, Published online: 22 Sep 2008

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Peter Ballard, Patrick Brassil, Khanh H. Bui, Hugues Dolgos, Carl Petersson, Anders Tunek & Peter J. H. Webborn. (2012) The right compound in the right assay at the right time: an integrated discovery DMPK strategy. Drug Metabolism Reviews 44:3, pages 224-252.
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Helen E. Cubitt, Karen R. Yeo, Eleanor M. Howgate, Amin Rostami-Hodjegan & Zoe E. Barter. (2011) Sources of interindividual variability in IVIVE of clearance: an investigation into the prediction of benzodiazepine clearance using a mechanistic population-based pharmacokinetic model. Xenobiotica 41:8, pages 623-638.
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N. Araki, S. Tsuruoka, N. Wang, G. Hasegawa, H. Yanagihara, H. Ando, T. Omasa, S. Enosawa, H. Nagai & A. Fujimura. (2008) Human CYP3A4-introduced HepG2 cells: screening system of new chemicals for the evaluation of CYP3A4-inhibiting activity. Xenobiotica 38:11, pages 1355-1364.
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Stefan S De Buck & Claire E Mackie. (2007) Physiologically based approaches towards the prediction of pharmacokinetics: in vitro–in vivo extrapolation. Expert Opinion on Drug Metabolism & Toxicology 3:6, pages 865-878.
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Carolina Noble, Niels Bjerre Holm, Marie Mardal & Kristian Linnet. (2018) Bromo-dragonfly, a psychoactive benzodifuran, is resistant to hepatic metabolism and potently inhibits monoamine oxidase A. Toxicology Letters 295, pages 397-407.
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P Ballard, P Brassil, K H Bui, H Dolgos, C Petersson, A Tunek & P J H Webborn. 2013. Drug Discovery and Development. Drug Discovery and Development 135 155 .
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R M Franke, C S Lancaster, C J Peer, A A Gibson, A M Kosloske, S J Orwick, R H Mathijssen, W D Figg, S D Baker & A Sparreboom. (2011) Effect of ABCC2 (MRP2) Transport Function on Erythromycin Metabolism. Clinical Pharmacology & Therapeutics 89:5, pages 693-701.
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Masato Chiba, Yasuyuki Ishii & Yuichi Sugiyama. (2009) Prediction of Hepatic Clearance in Human From In Vitro Data for Successful Drug Development. The AAPS Journal 11:2.
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Hege Christensen, Liv Mathiesen, Lillian W. Postvoll, Bjørn Winther & Espen Molden. (2009) Different Enzyme Kinetics of Midazolam in Recombinant CYP3A4 Microsomes from Human and Insect Sources. Drug Metabolism and Pharmacokinetics 24:3, pages 261-268.
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Peter J. Kilford, Rowan Stringer, Bindi Sohal, J. Brian Houston & Aleksandra Galetin. (2009) Prediction of Drug Clearance by Glucuronidation from in Vitro Data: Use of Combined Cytochrome P450 and UDP-Glucuronosyltransferase Cofactors in Alamethicin-Activated Human Liver Microsomes. Drug Metabolism and Disposition 37:1, pages 82-89.
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Alison J. Parker & J. Brian Houston. (2008) Rate-Limiting Steps in Hepatic Drug Clearance: Comparison of Hepatocellular Uptake and Metabolism with Microsomal Metabolism of Saquinavir, Nelfinavir, and Ritonavir. Drug Metabolism and Disposition 36:7, pages 1375-1384.
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John C. Lipscomb & Torka S. Poet. (2008) In vitro measurements of metabolism for application in pharmacokinetic modeling. Pharmacology & Therapeutics 118:1, pages 82-103.
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Michael Gertz, Peter J. Kilford, J. Brian Houston & Aleksandra Galetin. (2008) Drug Lipophilicity and Microsomal Protein Concentration as Determinants in the Prediction of the Fraction Unbound in Microsomal Incubations. Drug Metabolism and Disposition 36:3, pages 535-542.
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Matthew G. Soars, Dermot F. McGinnity, Ken Grime & Robert J. Riley. (2007) The pivotal role of hepatocytes in drug discovery. Chemico-Biological Interactions 168:1, pages 2-15.
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Trudy Rodgers & Malcolm Rowland. (2007) Mechanistic Approaches to Volume of Distribution Predictions: Understanding the Processes. Pharmaceutical Research 24:5, pages 918-933.
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Hayley S. Brown, Michael Griffin & J. Brian Houston. (2007) Evaluation of Cryopreserved Human Hepatocytes as an Alternative in Vitro System to Microsomes for the Prediction of Metabolic Clearance. Drug Metabolism and Disposition 35:2, pages 293-301.
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Bernard Testa & Stefanie D. Krämer. (2006) The Biochemistry of Drug Metabolism – An Introduction. Chemistry & Biodiversity 3:10, pages 1053-1101.
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Aleksandra Galetin & J. Brian Houston. (2006) Intestinal and Hepatic Metabolic Activity of Five Cytochrome P450 Enzymes: Impact on Prediction of First-Pass Metabolism. Journal of Pharmacology and Experimental Therapeutics 318:3, pages 1220-1229.
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Nancy Hakooz, Kiyomi Ito, Helen Rawden, Helen Gill, Lynn Lemmers, Alan R. Boobis, Robert J. Edwards, David J. Carlile, Brian G. Lake & J. Brian Houston. (2006) Determination of a Human Hepatic Microsomal Scaling Factor for Predicting in Vivo Drug Clearance. Pharmaceutical Research 23:3, pages 533-539.
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