Reactive drug metabolites
- 402 pages
- 15 hours of reading
This comprehensive introduction addresses a significant gap in the scientific literature, drawing from best practices in one of the largest pharmaceutical companies globally. The initial chapters explore the evolution of our understanding of drug metabolite toxicity, outlining fundamental concepts and techniques. The subsequent section focuses on chemical toxicophores associated with reactive metabolite formation and reviews drug-metabolizing enzymes involved in this process, including discussions on structure-toxicity relationships. Two chapters delve into contemporary issues surrounding herbal constituents and idiosyncratic adverse drug reactions (IADRs). Following this, the text presents current strategies to evaluate the reactive metabolite potential of new drug candidates through predictive and bioanalytical methods. An extensive analysis of the toxicological profiles of the top 200 prescription drugs illustrates the strengths and limitations of the toxicophore concept, supported by numerous case studies. The book concludes with a risk-benefit framework for managing the toxicity risks of drugs prone to reactive metabolites. Designed to build knowledge from basic principles to industry standards, it is accessible to medicinal chemists without extensive pharmacology training.
