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 1โ13): Scott J. Grossman
Chapter 2 Oxidative, Reductive, and Hydrolytic Metabolism of Drugs (pages 15โ35): F. Peter Guengerich
Chapter 3 Conjugative Metabolism of Drugs (pages 37โ88): Rory Remmel, Swati Nagar and Upendra Argikar
Chapter 4 Enzyme Kinetics (pages 89โ112): Timothy S. Tracy
Chapter 5 Metabolism?Mediated DrugโDrug Interactions (pages 113โ136): Hongjian Zhang, Michael W. Sinz and A. David Rodrigues
Chapter 6 Drug Transporters in Drug Disposition, Drug Interactions, and Drug Resistance (pages 137โ202): Cindy Q. Xia, Johnny J. Yang and Suresh K. Balani
Chapter 7 Regulatory Considerations of Drug Metabolism and Drug Interaction Studies (pages 203โ236): Xiaoxiong Wei and Mingshe Zhu
Chapter 8 Drug Metabolism Research as an Integral Part of the Drug Discovery Process (pages 237โ260): W. Griffith Humphreys
Chapter 9 Role of Drug Metabolism in Drug Development (pages 261โ285): Ramaswamy Iyer and Donglu Zhang
Chapter 10 Applications of Liquid Radiochromatography Techniques in Drug Metabolism Studies (pages 287โ317): Mingshe Zhu, Weiping Zhao and W. Griffith Humphreys
Chapter 11 Application of Liquid Chromatography/Mass Spectrometry for Metabolite Identification (pages 319โ367): Shuguang Ma and Swapan K. Chowdhury
Chapter 12 Introduction to NMR and Its Application in Metabolite Structure Determination (pages 369โ409): Xiaohua Huang, Robert Powers, Adrienne Tymiak, Robert Espina and Vikram Roongta
Chapter 13 Determination of Metabolic Rates and Enzyme Kinetics (pages 411โ446): Zhi?Yi Zhang and Laurence S. Kaminsky
Chapter 14 Protocols for Assessment of In vitro and In vivo Bioactivation Potential of Drug Candidates (pages 447โ476): Zhoupeng Zhang and Jinping Gan
Chapter 15 Reaction Phenotyping (pages 477โ512): Susan Hurst, J. Andrew Williams and Steven Hansel
Chapter 16 Analysis of In vitro Cytochrome P450 Inhibition in Drug Discovery and Development (pages 513โ544): Magang Shou and Renke Dai
Chapter 17 Testing Drug Candidates for CYP3A4 Induction (pages 545โ571): Gang Luo, Liang?Shang Gan and Thomas M. Guenthner
Chapter 18 ADME Studies in Animals and Humans: Experimental Design, Metabolite Profiling and Identification, and Data Presentation (pages 573โ604): Donglu Zhang and S. Nilgun Comezoglu