Handbook of Drug Metabolism, Third Edition  book cover
3rd Edition

Handbook of Drug Metabolism, Third Edition

ISBN 9780429190315
Published May 20, 2019 by CRC Press
750 Pages 150 B/W Illustrations

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Book Description

This book continues to be the definitive reference on drug metabolism with an emphasis on new scientific and regulatory developments. It has been updated based on developments that have occurred in the last 5 years, with new chapters on large molecules disposition, stereo-selectivity in drug metabolism, drug transporters and metabolic activation of drugs. Some chapters have been prepared by new authors who have emerged as subject area experts in the decade that has passed since publication of the first edition.

Key Features:

  • Continues to be the definitive reference on drug metabolism
  • Covers the drug transporter field, disposition of protein therapeutics and metabolic activation of drugs
  • Includes the contributions of world-class experts in their respective fields
  • Contains the work of editors who are recognized leaders and deep content experts in the field of drug metabolism
  • Emphasizes new scientific and regulatory developments in the field

Table of Contents

Section I: Fundamental Aspects of Drug Metabolism


Chapter 1: The Evolution of Drug Metabolism Research

Patrick J. Murphy

Chapter 2: Pharmacokinetics of Drug Metabolites

Philip C. Smith

Chapter 3: The Cytochrome P450 Oxidative System

Paul R. Ortiz de Montellano

Chapter 4: Aldehyde Oxidases an Emerging Group of Enzymes Involved in Xenobiotic Metabolism: Evolution, Structure, and Function

Enrico Garattini, Mineko Terao

Chapter 5: UDP-Glucuronosyltransferases

Robert S. Foti, Upendra A. Argikar


Section II: Factors Which Affect Drug Metabolism


Chapter 6: Non-CYP Drug Metabolizing Enzymes and Their Reactions

Shuguang Ma, Ryan H. Takahashi, Yong Ma, Sudheer Bobba, Donglu Zhang, S. Cyrus Khojasteh

Chapter 7: The Genetic Basis of Variation in Drug Metabolism and Toxicity

Tore Bjerregaard Stage, Deanna L. Kroetz

Chapter 8: Inhibition of Drug Metabolizing Enzymes

F. Peter Guengerich

Chapter 9: Quantitative Approaches to Human Clearance Projection in Drug Research and Development

Nigel J. Waters

Chapter 10: Sites of Extra Hepatic Metabolism, Part I: The Airways and Lung

John G. Lamb, Christopher A. Reilly

Chapter 11: Sites of Extra Hepatic Metabolism, Part II: Gut

Dan-Dan Tian, Emily J. Cox, Mary F. Paine

Chapter 12: Sites of Extra Hepatic Metabolism, Part III: Kidney

Lawrence H. Lash


Section III: Technologies to Study Drug Metabolism


Chapter 13: Mass Spectrometry in Drug Metabolism Research: Principles and Common Practice

Bo Wen

Chapter 14: The Role of NMR as a Qualitative and Quantitative Analytical Technique in Biotransformation Studies

Gregory S. Walker, Raman Sharma, Shuai Wang

Chapter 15: In Vitro Metabolism: Subcellular Fractions

Michael A. Mohutsy

Chapter 16: Drug Interaction Studies in the Drug Development Process: Studies In Vitro

R. Scott Obach, Kimberly Lapham

Chapter 17: Enzyme Induction Studies in Drug Discovery and Development

Joshua G. Dekeyser, Jan L. Wahlstrom

Chapter 18: Transporters in Drug Discovery and Development

Yaofeng Cheng, Yurong Lai

Chapter 19: Experimental Characterization of Cytochrome P450 Mechanism-Based Inhibition

Dan Rock, Michael Schrag, Larry C. Wienkers


Section IV: Applications of Metabolism Studies in Drug Discovery and Development


Chapter 20: Clinical Drug Metabolism

Kirk R. Henne, George R. Tonn, Bradley K. Wong

Chapter 21: Managing Metabolic Activation Issues in Drug Discovery

Sanjeev Kumar, Kaushik Mitra, Thomas A. Baillie

Chapter 22: Kinetic Differences between Generated and Preformed Metabolites: A Dilemma in Risk Assessment

Thomayant Prueksaritanont, Jiunn H. Lin

Chapter 23: Numerical Approaches to Drug Metabolism Kinetics and Pharmacokinetics

Ken Korzekwa, Swati Nagar

Chapter 24: Active Metabolites in Drug Development

Sylvie E. Kandel, Jed N. Lampe

Chapter 25: ADME of Antibody Drug Conjugates

Jiajie Yu, Cinthia Pastuskovas, Brooke M. Rock

Chapter 26: Managing Reactive Metabolites in Drug Discovery and Development

Amit S. Kalgutkar

Chapter 27: Applications of 14C Accelerator Mass Spectrometry in Drug Development

Raju Subramanian, Mark Seymour

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PAUL G. PEARSON is President and CEO, Pearson Pharma Partners, Westlake Village, California, USA. Dr. Pearson received his Ph.D. in Pharmaceutical Sciences from Aston University, Birmingham, UK. He has had an extensive and successful career in pharmaceutical science, previously serving as Vice President of Pharmacokinetics and Drug Metabolism at Amgen, Inc. and Executive Director of Preclinical Drug Metabolism at Merck & Co, Inc. He is an active member of several international and national professional organizations. Dr. Pearson has contributed to numerous peer-reviewed publications and has been an honored invited lecturer at conferences, society meetings, and symposia on drug development, drug metabolism, and drug discovery. Dr Pearson is actively engaged in the discovery and development of new human therapeutics to make a drammatic difference to the lives of patients.

LARRY C. WIENKERS is Principal Scientist, Wienkers Consulting, Bainbridge Island Washington, USA. Prior to consulting, Dr Wienkers served as Vice President of Pharmacokinetics and Drug Metabolism at Amgen, Inc. and Senior Director of Pharmacokinetics, Dynamics, and Metabolism at Pfizer. He obtained his Ph.D. in Medicinal Chemistry from the University of Washington, Seattle, Washington, USA and in 2014 he was awarded the University of Washington, School of Pharmacy Distinguished Alumni Award in Pharmaceutical Science and Research. Larry is a member of several professional societies, where he has served as Chair of American Society of Pharmacology and Experimental Therapeutics Division of Drug Metabolism and in 2013 was elected as Fellow in the American Association of Pharmaceutical Scientists. Dr. Wienkers has published over 80 peer-reviewed publications and book chapters has been an invited lecturer at conferences and symposia on large and small molecule drug metabolism and drug discovery.


The compendium is split into sections on; Fundamental aspects of drug metabolism, Factors which affect drug metabolism, Technologies to study drug metabolism, and Application of metabolism studies in drug discovery and development. Each chapter is well laid out with clear and useful figures and well referenced. As someone who wanted to know more about this field and having a basic knowledge, this was a good read. The chapters on enzyme inhibition and the genetic basis of variation in drug metabolism and toxicity were particularly good.

-Prof. Dudley E. Shallcross, University of Bristol, UK