Drug Metabolism in Drug Design and Development is a practical description of what happens during the drug design and development process and focuses on issues such as:

• what data are needed
• what experiments and analytical methods are typically employed
• how to interpret and apply data

Emphasizing facts, detailed experimental designs, applications, and limitations of techniques, the book contains four parts that integrate the entire process: basic principles, experimental designs, analytical methods, and data interpretation and application.

Features:

• Identifies and explains protocols for those professionals who are new to industrial drug development
• Brings users up to speed on the knowledge needed to conduct drug metabolic research
• Integrates the theoretical and practical aspects of drug metabolism, drug design, and drug development

Contents

Part I: Basic Concepts of Drug Metabolism

1. Overview: Drug Metabolism in the Modern Pharmaceutical Industry
2. Oxidative, Reductive, and Hydrolytic Metabolism of Drugs
3. Conjugative Metabolism of Drugs
4. Enzyme Kinetics
5. Metabolism-Mediated Drug–Drug Interactions
6. Drug Transporters in Drug Disposition, Drug Interactions, and Drug Resistance
7. Regulatory Considerations of Drug Metabolism and Drug Interaction Studies

Part II: Role of Drug Metabolism in the Pharmaceutical Industry

8. Drug Metabolism Research as an Integral Part of the Drug Discovery Process
9. Role of Drug Metabolism in Drug Development

Part III: Analytical Techniques in Drug Metabolism

10. Applications of Liquid Radiochromatography Techniques in Drug Metabolism Studies
11. Application of Liquid Chromatography/Mass Spectrometry for Metabolite Identification
12. Introduction to NMR and Its Application in Metabolite Structure Determination

Part IV: Common Experimental Approaches and Protocols

13. Determination of Metabolic Rates and Enzyme Kinetics
14. Protocols for Assessment of In vitro and In vivo Bioactivation Potential of Drug Candidates
15. Reaction Phenotyping
16. Analysis of In vitro Cytochrome P450 Inhibition in Drug Discovery and Development
17. Testing Drug Candidates for CYP3A4 Induction
18. ADME Studies in Animals and Humans: Experimental Design, Metabolite Profiling and Identification, and Data Presentation

Index

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