This book examines the background, industrial context, process, analytical methodology, and technology of metabolite identification. It emphasizes the applications of metabolite identification in drug research. While primarily a textbook, the book also functions as a comprehensive reference to those in the industry.

Foreword (Tom Baillie). Preface (Mike Lee and Mingshe Zhu). Contributors. Part I. Basic Concepts of Drug Metabolism and Disposition. 1. Progression of Drug Metabolism (Ronald E. White). 2. Common Biotransformation Reactions (Bo Wen and Sidney D. Nelson). 3. Metabolic Activation of Organic Functional Groups Utilized in Medicinal Chemistry (Amit S. Kalgutkar). 4. Drug-Metabolizing Enzymes, Transporters, and Drug-Drug Interactions (Steven W. Louie and Magang Shou). 5. Experimental Models of Drug Metabolism and Disposition (Gang Luo, Chuang Lu, Xinxin Ding, and Donglu Zhang). 6. Principles of Pharmacokinetics: Predicting Human Pharmacokinetics in Drug Discovery (Takehito Yamamoto, Akihiro Hisaka, and Hiroshi Suzuki). 7. Drug Metabolism Research as Integral Part of Drug Discovery and Development Processes (W. Griffith Humphereys). Part II. Mass Spectrometry in Drug Metabolism: Principles and Common Practice. 8. Theory and Instrumentation of Mass Spectrometry (Gérard Hopfgartner). 9. Common Liquid Chromatography-Mass Spectrometry (LC-MS) Methodology for Metabolite Identification (Lin Xu, Lewis J. Klunk, and Chandra Prakash). 10. Mass Spectral Interpretation (Li-Kang Zhang and Birendra N. Pramanik). 11. Techniques to Facilitate the Performance of Mass Spectrometry: Sample Preparation, Liquid Chromatography, and Non-Mass-Spectrometric Detection (Mark Hayward, Maria D. Bacolod, Qing Ping Han, Manuel Cajina, and Zack Zou). Part III. Applications of New LC-MS Techniques in Drug Metabolism and Disposition. 12. Quantitative In Vitro ADME Assays Using LC-MS as a Part of Early Drug Metabolism Screening (Walter Korfmacher). 13. High-Resolution Mass Spectrometry and Drug Metabolite Identification (Russell J. Mortishire-Smith, Haiying Zhang, and Kevin P. Bateman). 14. Distribution Studies of Drugs and Metabolites in Tissue by Mass Spectrometric Imaging (Richard F. Reich, Daniel P. Magparangalan, Timothy J. Garrett, and Richard A. Yost). 15. Use of Triple Quadrupole-Linear Ion Trap Mass Spectrometry as a Single LC-MS Platform in Drug Metabolism and Pharmacokinetics (Wenying Jian, Ming Yao, Bo Wen, Elliott B. Jones, and Mingshe Zhu). 16. Quantitative Drug Metabolism with Accelerator Mass Spectrometry (John S. Vogel, Peter Lohstroh, Brad Keck, and Stephen R. Dueker). 17. Standard-Free Estimation of Metabolite Levels Using Nanospray Mass Spectrometry: Current Statutes and Future Directions (Jing-Tao Wu). 18. Profiling and Characterization of Herbal Medicine and Its Metabolites Using LC-MS (Zeper Abliz, Ruiping Zhang, Ping Geng, Dongmei Dai, Jiuming He, and Jian Liu). 19. Liquid Chromatography Mass Spectrometry Bioanalysis of Protein Therapeutics and Biomarkers in Biological Matrices (Fumin Li and Qin C. Ji). 20. Mass Spectrometry in the Analysis of DNA, Protein, Peptide, and Lipid Biomarkers of Oxidative Stress (Stacy L. Gelhaus and Ian A. Blair). 21. LC-MS in Endogenous Metabolite Profiling and Small-Molecule Biomarker Discovery (Michael D. Reily, Petia Shipkova, and Serhiy Hnatyshyn). Appendix. Index.  

The pioneering guide to solving real-world problems in drug metabolism using mass spectrometry Mass spectrometry has become the predominant analytical tool for drug metabolism and pharmacokinetics research in modern drug discovery and development. This book represents a coherent integration of all relevant background knowledge and detail surrounding the analytical technologies in this new multidisciplinary field. With chapters written by internationally renowned authors, the book provides details on: Basic concepts of drug metabolism and pharmacokineticsThe principles and common practice of mass spectrometry in drug metabolismApplications of new LC/MS techniques in drug metabolism and disposition Mass Spectrometry in Drug Metabolism and Disposition examines fundamental aspects and practical considerations of using mass spectrometry in drug metabolism such as biotransformation reactions, metabolizing enzymes, transporters and drug-drug interactions, drug metabolism in drug design and development, theory and instrumentation of mass spectrometry, and LC/MS approaches to drug metabolism and mass spectral interpretation. Exciting details on new mass spectrometry technology and novel applications used in the frontiers of pharmaceutical research, including high-resolution mass spectrometry in metabolite identification, imaging mass spectrometry in drugtissue distribution, accelerator mass spectrometry in microdosing, as well as theanalyses of metabolomes, herbal medicine, biomarkers, and biologics by various mass spectrometers are also highlighted in the book. This unique book serves as both a textbook for students as well as a comprehensive reference for pharmaceutical professionals, offering fresh and exciting solutions in the ongoing effort to design and develop drugs that are both effective and safe.

"It is a state-of-the-art and mostly comprehensive overview of the field. It will be a valuable source of information for all those who want to start in the fields of drug metabolism and MS, e.g., PhD students, but also senior scientists, etc."  (Analytical and Bioanalytical Chemistry, 31 July 2012) "Overall, Mass Spectrometry in Drug Metabolism and Pharmacokinetics is a valuable and interesting resource for a broad readership, including scientists starting to work in DMPK as well as undergraduate and graduate students getting involved in drug discovery and characterization by means of MS." (J Am Soc Mass Spectrom, 2011) "Placing the imaging technology in the context of the principles and applications of drug design, the book can serve as a textbook for either field." (Book New, 1 August 2011)