Handbook of Drug Metabolism provides comprehensive coverage of the fundamental aspects of drug metabolism and the practical applications that help guide researchers through key challenges in modern drug discovery and development.

This Second edition covers the many recent scientific and technical advances in the field and is organized into four sections:

• fundamental aspects of drug metabolism
• factors that affect drug metabolism
• new enabling technologies to study drug metabolism
• applications of metabolism studies in drug development and drug discovery

Contents

Part I: Fundamental Aspects of Drug Metabolism

1. The Evolution of Drug Metabolism Research
2. Pharmacokinetics of Drug Metabolites
3. Hepatic Architecture: Functional and Subcellular Correlates
4. The Cytochrome P450 Oxidative System
5. Transformation Enzymes: Oxidative; Non-P450
6. UDP-Glucuronosyltransferases

Part II: Factors Which Affect Drug Metabolism

7. Pharmacogenetics
8. Inhibition of Drug Metabolizing Enzymes
9. The Ontogeny of Drug Metabolizing Enzymes/Pediatric Exclusivity
10. Sites of Extra Hepatic Metabolism, Part I: Lung
11. Sites of Extra Hepatic Metabolism, Part II: Gut
12. Sites of Extra Hepatic Metabolism, Part III: Kidney
13. Sites of Extra Hepatic Metabolism, Part IV: Brain

Part III: Technologies to Study Drug Metabolism

14. LC-MS Analysis in Drug Metabolism Studies
15. The Practice of NMR Spectroscopy in Drug Metabolism Studies
16. Applications of Recombinant and Purified Human Drug-Metabolizing Enzymes: An Industrial Perspective
17. In Vitro Metabolism: Subcellular Fractions
18. In Vitro Metabolism: Hepatocytes
19. Drug Interaction Studies in the Drug Development Process: Studies In Vitro
20. Enzyme Induction Studies in Drug Discovery & Development
21. Experimental Characterization of Cytochrome P450 Mechanism Based Inhibition

Part IV: Applications of Metabolism Studies in Drug Discovery and Development

22. Clinical Drug Metabolism
23. Minimizing Metabolic Activation in Drug Discovery
24. Kinetic Differences between Generated and Preformed Metabolites: A Dilemma in Risk Assessment
25. The Use of Transgenic Animals to Study Drug Metabolism
26. Preclinical Pharmacokinetic Models for Drug Discovery and Development

Index

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