1st Edition

Drug Metabolizing Enzymes Cytochrome P450 and Other Enzymes in Drug Discovery and Development

Edited By Jae Lee, R. Scott Obach, Michael B. Fisher Copyright 2003

    Critical in the elimination of drugs and other xenobiotics from the body, cytochrome P450 has strong bearing on scientific assessments of genetic polymorphism in metabolism, possible drug-drug interactions, and bioavailability of candidate drugs. This text systematizes findings on P450 and similar enzymes - as well as parallel issues shaping the pharmaceutical industry - to promote the next generation of safer, more effective drugs.

    Dioxygen activation by cytochromes P450 - a role for multiple oxidants in the oxidation of substrates, Alfin D.N. Vaz; application of LC/MS, LC/NMR, NMR and stable isotopes in identifying and characterizing metabolites, A.E. Mutlib and John P. Shockcor; bioactivation, Jack Uetrecht; chemically reactive metabolites in drug discovery and development, Thomas A. Baillie; cytochrome P450 and its place in drug discovery and development, Dennis Smith; cytochrome P450 in laboratory animal species, Margit Spatzenegger, Stephanie L. Born and James R. Halpert; typical and atypical enzyme, Kinetics J. Brian Houston, Kathryn E. Kenworthy and Aleksandra Galetin; cytochrome P450 reaction phenotyping, Larry C. Wienkers and Jeffrey C. Stevens; drug-drug interactions and the cytochromes P450, Kenneth A. Bachmann, Barbara J. Ring and Steven A. Wrighton; CYP gene induction by xenobiotics and drugs, Jean-Marc Pascussi, Sabine Gerbal-Chaloin, Martine Daujat, Lionel Drocourt, Lydiane Pichard-Garcia, Marie-Jose Vilarem, Patrick Maurel, Sylvie Klieber, Francois Torreilles, Martine Bourrie, Francois Guillou and Gerard Fabre; cytochrome P450 pharmacogenetics, Robert L. Haining and Aiming Yu; role of intestinal cytochromes P450 in drug deposition, Mary F. Paine and Kenneth E. Thummel; prediction of hepatic clearance in humans from experimental animals and in vitro data, Masato Chiba, Yoshihiro Shibata, Hiroyuki Takahashi, Yasuyuki Ishii and Yuichi Sugiyama; non-P450 mediated oxidative metabolism of xenobiotics, Dieter Lang and Amit S. Kalgutkar; the role of sulfotransferases (SULTs) and UDP-glucuronosyltransferases (UGTs) in human drug clearance and bioactivation, Michael W.H. Coughtrie and Michael B. Fisher.


    Jae Lee, R. Scott Obach, Michael B. Fisher