Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6.

作者: Zeruesenay Desta , Bryan A. Ward , Nadia V. Soukhova , David A. Flockhart

DOI: 10.1124/JPET.104.065607

关键词:

摘要: We performed comprehensive kinetic, inhibition, and correlation analyses in human liver microsomes and experiments in expressed human cytochromes P450 (P450s) to identify …

参考文章(42)
Andreas Nüssler, Peter Neuhaus, Ulrich M. Zanger, Michel Eichelbaum, Thomas E. Mürdter, Janet K. Coller, Niels Krebsfaenger, Kathrin Klein, Karin Endrizzi, Renzo Wolbold, Thomas Lang, The influence of CYP2B6, CYP2C9 and CYP2D6 genotypes on the formation of the potent antioestrogen Z-4-hydroxy-tamoxifen in human liver. British Journal of Clinical Pharmacology. ,vol. 54, pp. 157- 167 ,(2002) , 10.1046/J.1365-2125.2002.01614.X
J.L. Borgna, H. Rochefort, Hydroxylated metabolites of tamoxifen are formed in vivo and bound to estrogen receptor in target tissues. Journal of Biological Chemistry. ,vol. 256, pp. 859- 868 ,(1981) , 10.1016/S0021-9258(19)70058-1
Janet K. Coller, Niels Krebsfaenger, Kathrin Klein, Renzo Wolbold, Andreas Nüssler, Peter Neuhaus, Ulrich M. Zanger, Michel Eichelbaum, Thomas E. Mürdter, Large interindividual variability in the in vitro formation of tamoxifen metabolites related to the development of genotoxicity British Journal of Clinical Pharmacology. ,vol. 57, pp. 105- 111 ,(2003) , 10.1046/J.1365-2125.2003.01970.X
David Kupfer, Shangara S. Dehal, CYP2D6 catalyzes tamoxifen 4-hydroxylation in human liver. Cancer Research. ,vol. 57, pp. 3402- 3406 ,(1997)
P E Lłnning, G K Poon, M G Rowlands, M Jarman, Y C Chui, R Feng, R McCague, Analysis of phase I and phase II metabolites of tamoxifen in breast cancer patients. Drug Metabolism and Disposition. ,vol. 21, pp. 1119- 1124 ,(1993)
Per M. Ueland, Einar Solheim, Ernst A. Lien, Distribution of tamoxifen and its metabolites in rat and human tissues during steady-state treatment. Cancer Research. ,vol. 51, pp. 4837- 4844 ,(1991)
V. Craig Jordan, C. Chem., Metabolites of tamoxifen in animals and man: Identification, pharmacology, and significance Breast Cancer Research and Treatment. ,vol. 2, pp. 123- 138 ,(1982) , 10.1007/BF01806449
Françoise Jacolot, Isabelle Simon, Yvonne Dreano, Philippe Beaune, Christian Riche, François Berthou, Identification of the cytochrome P450 IIIA family as the enzymes involved in the N-demethylation of tamoxifen in human liver microsomes. Biochemical Pharmacology. ,vol. 41, pp. 1911- 1919 ,(1991) , 10.1016/0006-2952(91)90131-N