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.

• Reviews the analytical techniques and experimental designs critical for metabolite studies
• Covers methods including chirality, species differences, mass spectrometry, radiolabels, and in vitro / in vivo correlation
• Discusses target pharmacology, in vitro systems aligned to toxicity tests, and drug-drug interactions
• Includes perspectives from authors with firsthand involvement in industry and the study of drug metabolites, including viewpoints that have influenced regulatory guidelines

Table of Contents

Chapter 1 Introduction: History of Metabolite Safety in Drug Development
Chapter 2 “mist” And Other Metabolite Guidelines In The Context Of Industrial Drug Metabolism
Chapter 3 Metabolite Technology: Qualitative and Quantitative
Chapter 4 In Vitro Methods For Evaluation Of Drug Metabolism: Identification Of Active And Inactive Metabolites And The Enzymes That Generate Them
Chapter 5 Integrated Reactive Metabolite Strategies
Chapter 6 Understanding Drug Metabolism in Humans: In Vivo
Chapter 7 Topical Administration and Safety Testing of Metabolites
Chapter 8 In Silico Modeling of Metabolite Kinetics
Chapter 9 Introduction to Case Studies
Chapter 10 A Mass Balance And Metabolite Profiling Study Of Sonidegib In Healthy Male Subjects Using Microtrace Approach
Chapter 11 Dealing With Reality: When Is It Necessary To Qualify And Quantify Metabolites? Some Case Studies
Chapter 12 The Value Of Metabolite Identification And Quantification In Clinical Studies. Some Case Studies Enabling Early Assessment Of Sa
Chapter 13 The Importance Of Doseand Time-dependent Pharmacokinetics During Early Metabolite Safety Assessment In Humans
Chapter 14 Mist and the Future