Drug Metabolism in Drug Design and Development: Basic Concepts and Practice
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Description
The essentials of drug metabolism vital to developing new therapeutic entities Information on the metabolism and disposition of candidate drugs is a critical part of all aspects of the drug discovery and development process. Drug metabolism, as practiced in the pharmaceutical industry today, is a complex, multidisciplinary field that requires knowledge of sophisticated analytical technologies and expertise in mechanistic and kinetic enzymology, organic reaction mechanism, pharmacokinetic analysis, animal physiology, basic chemical toxicology, preclinical pharmacology, and molecular biology. With chapters contributed by experts in their specific areas, this reference covers: * Basic concepts of drug metabolism * The role of drug metabolism in the pharmaceutical industry * Analytical techniques in drug metabolism * Common experimental approaches and protocols Drug Metabolism in Drug Design and Development emphasizes practical considerations such as the data needed, the experiments and analytical methods typically employed, and the interpretation and application of data. Chapters highlight facts, common protocols, detailed experimental designs, applications, and limitations of techniques. This is a comprehensive, hands-on reference for drug metabolism researchers as well as other professionals involved in pre-clinical drug discovery and development.Content: Chapter 1 Overview: Drug Metabolism in the Modern Pharmaceutical Industry (pages 1–13): Scott J. GrossmanChapter 2 Oxidative, Reductive, and Hydrolytic Metabolism of Drugs (pages 15–35): F. Peter GuengerichChapter 3 Conjugative Metabolism of Drugs (pages 37–88): Rory Remmel, Swati Nagar and Upendra ArgikarChapter 4 Enzyme Kinetics (pages 89–112): Timothy S. TracyChapter 5 Metabolism?Mediated Drug–Drug Interactions (pages 113–136): Hongjian Zhang, Michael W. Sinz and A. David RodriguesChapter 6 Drug Transporters in Drug Disposition, Drug Interactions, and Drug Resistance (pages 137–202): Cindy Q. Xia, Johnny J. Yang and Suresh K. BalaniChapter 7 Regulatory Considerations of Drug Metabolism and Drug Interaction Studies (pages 203–236): Xiaoxiong Wei and Mingshe ZhuChapter 8 Drug Metabolism Research as an Integral Part of the Drug Discovery Process (pages 237–260): W. Griffith HumphreysChapter 9 Role of Drug Metabolism in Drug Development (pages 261–285): Ramaswamy Iyer and Donglu ZhangChapter 10 Applications of Liquid Radiochromatography Techniques in Drug Metabolism Studies (pages 287–317): Mingshe Zhu, Weiping Zhao and W. Griffith HumphreysChapter 11 Application of Liquid Chromatography/Mass Spectrometry for Metabolite Identification (pages 319–367): Shuguang Ma and Swapan K. ChowdhuryChapter 12 Introduction to NMR and Its Application in Metabolite Structure Determination (pages 369–409): Xiaohua Huang, Robert Powers, Adrienne Tymiak, Robert Espina and Vikram RoongtaChapter 13 Determination of Metabolic Rates and Enzyme Kinetics (pages 411–446): Zhi?Yi Zhang and Laurence S. KaminskyChapter 14 Protocols for Assessment of In vitro and In vivo Bioactivation Potential of Drug Candidates (pages 447–476): Zhoupeng Zhang and Jinping GanChapter 15 Reaction Phenotyping (pages 477–512): Susan Hurst, J. Andrew Williams and Steven HanselChapter 16 Analysis of In vitro Cytochrome P450 Inhibition in Drug Discovery and Development (pages 513–544): Magang Shou and Renke DaiChapter 17 Testing Drug Candidates for CYP3A4 Induction (pages 545–571): Gang Luo, Liang?Shang Gan and Thomas M. GuenthnerChapter 18 ADME Studies in Animals and Humans: Experimental Design, Metabolite Profiling and Identification, and Data Presentation (pages 573–604): Donglu Zhang and S. Nilgun Comezoglu
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