Drug Metabolism in Drug Design and Development (eBook)

Donglu Zhang, PhD, is a senior scientist in the Biotransformation Depart-ment at Bristol-Myers Squibb. His research interests include metabolite characterization, drug metabolism enzymology, LC/MS methodologies, and microbial biotransformation. MINGSHE ZHU, PhD, is a drug metabolism scientist with more than ten years of experience in drug discovery and development. His research interests include metabolic activation, LC/MS technology, and regulatory drug metabolism. W. Griffith Humphreys, PhD, is the Director of the Biotransformation Department at Bristol-Myers Squibb. His research interests include optimizationof ADME properties, metabolic activation, and new methodologies for metabolite characterization.

Preface.

Contributors.

Part I: Basic Concepts of Drug Metabolism.

1. Overview: Drug Metabolism in the Modern Pharmaceutical
Industry (Scott J. Grossman)

2. Oxidative, Reductive, and Hydrolytic Metabolism of Drugs (F.
Peter Guengerich)

3. Conjugative Metabolism of Drugs (Rory Remmel, Swati Nagar and
Upendra Argikar)

4. Enzyme Kinetics (Timothy S. Tracy)

5. Metabolism-Mediated Drug-Drug Interactions (Hongjian Zhang,
Michael W. Sinz, and A. David Rodrigues)

6. Drug Transporters in Drug Disposition, Drug Interactions, and
Drug Resistance (Cindy Q. Xia, Johnny J. Yang, and Suresh K.
balani)

7. Regulatory Considerations of Drug Metabolism and Drug
Interaction Studies (Xiaoxiong Wei and Mingshe Zhu)

Part II: Role of Drug Metabolism in the Pharmaceutical
Industry.

8. Drug Metabolism Research as an Integral Part of the Drug
Discovery Process (W. Griffith Humphreys)

9. Role of Drug Metabosim in Drug Development (Ramaswamy Iyer
and Donglu Zhang)

Part III: Analytical techniques in Drug Metabolism.

10. Applications of Liquid Radiochromatography Techniques in
Drug Metabolism Studies (Mingshe Zhu, Weiping Zhao, and W. Griffith
Humphreys)

11. Application of Liquid Chromatogrpahy/Mass Spectrometry for
Metabolite Identification (Shuguang Ma and Swapan K. Chowdhury)

12. Introductin to NMR and Its Application in Metabolite
Structure Determination (Xiaohua Huang, Robert Powers, Adrienne
Tymiak, Robert Espina, and Vikram Roongta)

Part IV: Common Experimental Approaches and
Protocols.

13. Determination of Metabolic Rats and Enzyme Kinetics (Zhi-Yi
Zhang and Laurence S. Kaminsky)

14. Protocols for Assessment of In vitro and In vivo
Bioactivation Potential of Drug Candidates (Zhoupeng Zhang and
Jinping Gan)

15. Reaction Phenotyping (Susan Hurst, J. Andrew Williams, and
Steven Hansel)

16. Analysis of In vitro Cytochrome P450 Inhibition in Drug
Discovery and Development (Magang Shou and Renke Dai)

17. Testing Drug Candidates for CYP3A4 Induction (Gang Luo,
Liang-Shang Gan, and Thomas M. Guenthner)

18. ADME Studies in Animals and Humans: Experimental Design,
Metabolite Profoling and Identification, and Data Presentation
(Donglu Zhang and S. Nilgun Comezoglu)

Index.

"I highly recommend this book to anyone interested in drug metabolism." (Journal of Medicinal Chemistry, 2008)