Reactive metabolites, new modalities, and regulatory guidance for drug development

Drug Metabolism and Biotransformation: Enzymes, Approaches, New Modalities, Special Populations, and Challenges in Drug Development addresses practical biotransformation challenges that pharma and biopharma scientists face during preclinical and clinical development. Beginning with a historical perspective, drug metabolizing enzymes, and reactive metabolites, , the book progresses through emerging technologies and metabolite synthesis to industry challenges including drug-drug interactions, and extrahepatic metabolism including microbiota.

Drug Metabolism and Biotransformation extends beyond traditional small molecules to coverPROTACs, peptides, proteins, ADCs and oligonucleotides, detailing how metabolism study scope differs for these drug modalities. The book incorporates case studies, interviews with biotransformation scientists, regulatory guidance from FDA, ICH, and sections addressing drug metabolism in real-life patient populations.

Readers will also find:

• Interviews with experienced biotransformation scientists offering perspectives on solving complex metabolism problems encountered during drug development
• Detailed coverage of metabolite synthesis approaches critical for structural characterization and quantitative assessment of metabolites of interest
• Practical discussion of preclinical-to-clinical translation challenges including species differences and human-relevant metabolite identification strategies
• Guidance for navigating regulatory requirements across major international bodies governing metabolite safety and drug-drug interaction studies
• Special population pharmacology extending drug metabolism analysis beyond standard clinical frameworks

Written for medicinal chemists, biotransformation scientists in the pharma and biopharma industry, drug discovery and development professionals, toxicologists, and analytical chemists, this book provides the practical biotransformation knowledge needed to address metabolism challenges from early discovery through regulatory submission and post-market considerations.

Emre M. Isin, PhD, trained as an organic chemist is currently the Head of the Global DMPK Department at Servier, having previously held positions at UCB Biopharma and AstraZeneca. He is one of the founding members and co-organizer of the European Biotransformation Workshops, contributing to the advancement of drug metabolism science across the pharmaceutical industry.

Markus Walles, PhD, is the Global Head of Biotransformation within the Department of Pharmacokinetic Sciences at Novartis where he developed deep expertise in biotransformation science spanning from both preclinical and clinical stages of drug development programs. He previously held a research position at AstraZeneca and is also one of the founding members and co-organizer of the European Biotransformation Workshops driving the advancement of drug metabolism science across the pharmaceutical industry.