Metabolite safety in drug development

"A reference on drug metabolism and metabolite safety in the development phase, this book reviews the analytical techniques and experimental designs critical for metabolite studies. It features case studies of lessons learned and real world examples, along with regulatory perspectives from the US FDA and EMA. & bull; Reviews the analytical techniques and experimental designs critical for metabolite studies & bull; Covers methods including chirality, species differences, mass spectrometry, radiolabels, and in vitro / in vivo correlation & bull; Discusses target pharmacology, in vitro systems aligned to toxicity tests, and drug-drug interactions & bull; Includes perspectives from authors with firsthand involvement in industry and the study of drug metabolites, including viewpoints that have influenced regulatory guidelines"--

"This book focuses on the characterization of metabolites once a drug candidate is selected, featuring case studies to illustrate lessons learned and a perspective on future directions"--

Machine generated contents note: PREFACE LIST OF CONTRIBUTORS 1. Introduction: History of Metabolite Safety in Drug Development Dennis A. Smith and Suzanne L. Iverson 1.1. People, events and reaction 1.2. The rise of industrial drug metabolism 1.3. The appearance of MIST 1.4. The journey triggered by thalidomide- would present science have made a difference? 1.5. Key events from thalidomide to MIST 1.6. The purpose of this book 1.7. References 2. "MIST" and other metabolite guidelines in the context of industrial drug metabolism Gordon J. Dear and Angus N.R. Nedderman 2.1. A historical perspective 2.2. The emergence of the regulatory guidance documents 2.3. Impact of the guidelines 2.4. Future directions? 2.5. References 3. Metabolite technology -- qualitative and quantitative Gordon J. Dear and Andrew McEwen 3.1. Introduction 3.2. Clinical Samples 3.3. Pre-Clinical Samples 3.4. Radiolabelled test compounds 3.5. Mass Spectrometry 3.6. Nuclear magnetic resonance Spectroscopy 3.7. Accelerator mass spectrometry (AMS) 3.8. Further Reading 3.9. References 4. In Vitro methods for evaluation of drug metabolism: Identification of active and inactive metabolites and the enzymes that genera…