With practical details informed by leading drug metabolism specialists in industry and academic research, Drug Metabolizing Enzymes considers:

• dioxygen activation by P450
• characterization of metabolites through LC/MS, LC/NMR, NMR, and stable isotope techniques
• P450 in experimental animals
• bioactivation and human drug clearance
• enzyme kinetics and P450 reaction Phenotyping
• pharmacogenetics and P450 gene induction by xenobiotics and by drugs
• the influence of intestinal cytochrome P450 on drug disposition
• P450 in drug-drug interactions
• non-P450 mediated metabolism of xenobiotics

Contents

1. Dioxygen Activation by Cytochromes P450: A Role for Multiple Oxidants in the Oxidation of Substrates
2. Application of LC/MS, LC/NMR, NMR and Stable Isotopes in Identifying and Characterizing Metabolites
3. Bioactivation
4. Chemically Reactive Metabolites in Drug Discovery and Development
5. Cytochrome P450 and its Place in Drug Discovery and Development
6. Cytochrome P450 in Laboratory Animal Species
7. Typical and Atypical Enzyme Kinetics
8. cytochrome P450 Reaction Phenotyping
9. Drug-Drug Interactions and the Cytochromes P450
10. CYP Gene Induction by Xenobiotics and Drugs
11. Cytochrome P450 Pharmacogenetics
12. Role of Intestinal Cytochromes P450 in Drug Disposition
13. Prediction of Hepatic Clearance in humans from Experimental Animals and In Vitro Data
14. Non-P450 Mediated Oxidative Metabolism of Xenobiotics
15. The Role of Sulfotransferases (SULTS) and UDP-glucuronosyltransferases (UGTS) in Human Drug Clearance and Bioactivation

Index

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