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Xenobiotica
the fate of foreign compounds in biological systems
Volume 29, 1999 - Issue 3
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Research Article

Utility of hepatocytes to model species differences in the metabolism of loxtidine and to predict pharmacokinetic parameters in rat, dog and man

Pages 253-268 | Published online: 22 Sep 2008

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Qiuping Ye, Min Jiang, Wotang T. Huang, Yun Ling, Steven H. Olson, Daqing Sun, Guifen Xu, Xuelei Yan, Bradley K. Wong & Lixia Jin. (2015) Pharmacokinetics and metabolism of AMG 232, a novel orally bioavailable inhibitor of the MDM2–p53 interaction, in rats, dogs and monkeys: in vitro–in vivo correlation. Xenobiotica 45:8, pages 681-692.
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Vicki M. Richardson, Stephen S. Ferguson, Yusupha M. Sey & Michael J. DeVito. (2014) In vitro metabolism of thyroxine by rat and human hepatocytes. Xenobiotica 44:5, pages 391-403.
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Qinghua Wu, Lingli Huang, Zhaoying Liu, Min Yao, Yulian Wang, Menghong Dai & Zonghui Yuan. (2011) A comparison of hepatic in vitro metabolism of T-2 toxin in rats, pigs, chickens, and carp. Xenobiotica 41:10, pages 863-873.
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Brandon Swift*Nathan D. Pfeifer*Kim L.R. Brouwer. (2010) Sandwich-cultured hepatocytes: an in vitro model to evaluate hepatobiliary transporter-based drug interactions and hepatotoxicity. Drug Metabolism Reviews 42:3, pages 446-471.
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R. Smith, R. D. O. Jones, P. G. Ballard & H. H. Griffiths. (2008) Determination of microsome and hepatocyte scaling factors for / extrapolation in the rat and dog. Xenobiotica 38:11, pages 1386-1398.
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Nicola J. Hewitt, María José Gómez Lechón, J. Brian Houston, David Hallifax, Hayley S. Brown, Patrick Maurel, J. Gerald Kenna, Lena Gustavsson, Christina Lohmann, Christian Skonberg, Andre Guillouzo, Gregor Tuschl, Albert P. Li, Edward LeCluyse, Geny M. M. Groothuis & Jan G. Hengstler. (2007) Primary Hepatocytes: Current Understanding of the Regulation of Metabolic Enzymes and Transporter Proteins, and Pharmaceutical Practice for the Use of Hepatocytes in Metabolism, Enzyme Induction, Transporter, Clearance, and Hepatotoxicity Studies. Drug Metabolism Reviews 39:1, pages 159-234.
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D. M. CROSS & M. K. BAYLISS. (2000) A COMMENTARY ON THE USE OF HEPATOCYTES IN DRUG METABOLISM STUDIES DURING DRUG DISCOVERY AND DEVELOPMENT*. Drug Metabolism Reviews 32:2, pages 219-240.
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N. J. Hewitt, T. Fischer, U. Zuehlke, F. Oesch & D. Utesch. (2000) Metabolic activity of fresh and cryopreserved cynomolgus monkey (Macaca fascicularis) hepatocytes. Xenobiotica 30:7, pages 665-681.
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Esther F.A Brandon, Christiaan D Raap, Irma Meijerman, Jos H Beijnen & Jan H.M Schellens. (2003) An update on in vitro test methods in human hepatic drug biotransformation research: pros and cons. Toxicology and Applied Pharmacology 189:3, pages 233-246.
Crossref
Yoichi Naritomi, Shigeyuki Terashita, Akira Kagayama & Yuichi Sugiyama. (2003) Utility of Hepatocytes in Predicting Drug Metabolism: Comparison of Hepatic Intrinsic Clearance in Rats and Humans in Vivo and in Vitro. Drug Metabolism and Disposition 31:5, pages 580-588.
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N. Le Goff, J. C. Koffel, S. Vandenschrieck, L. Jung & G. Ubeaud. (2002) Comparison of in vitro hepatic models for the prediction of metabolic interaction between simvastatin and naringenin. European Journal of Drug Metabolism and Pharmacokinetics 27:4, pages 233-241.
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Katrin Zeilinger, Igor M. Sauer, Gesine Pless, Catrin Strobel, Jeannette Rudzitis, Aiguo Wang, Andres K. Nüssler, Alexander Grebe, Lei Mao, Stefan H.G. Auth, Juliane Unger, Peter Neuhaus & Jörg C. Gerlach. (2002) Three-dimensional Co-culture of Primary Human Liver Cells in Bioreactors for In Vitro Drug Studies: Effects of the Initial Cell Quality on the Long-term Maintenance of Hepatocyte-specific Functions . Alternatives to Laboratory Animals 30:5, pages 525-538.
Crossref
T. Lavé, O. Luttringer, J. Zuegge, G. Schneider, P. Coassolo & F.-P. Theil. 2002. Pharmacokinetic Challenges in Drug Discovery. Pharmacokinetic Challenges in Drug Discovery 81 104 .
Margherita Strolin Benedetti. (2001) Biotransformation of xenobiotics by amine oxidases. Fundamental & Clinical Pharmacology 15:2, pages 75-84.
Crossref
Genevieve Ubeaud, Claus-Ditter Schiller, Fabrice Hurbin, Daniel Jaeck & Philippe Coassolo. (2001) Comparison of the stability of some major cytochrome P450 and conjugation reactions in rat, dog and human hepatocyte monolayers. European Journal of Drug Metabolism and Pharmacokinetics 26:1-2, pages 37-45.
Crossref
Jochen Zuegge, Gisbert Schneider, Philippe Coassolo & Thierry Lav??. (2001) Prediction of Hepatic Metabolic Clearance. Clinical Pharmacokinetics 40:7, pages 553-563.
Crossref
Martin K. Bayliss & David M. Cross. 2000. The Hepatocyte Review. The Hepatocyte Review 365 389 .

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