This book overviews the various facets of polypharmacology, with emphasis on practical aspects, such as how to address adverse polypharmacology or how to approach the discovery of polypharmacological drugs. These two (somewhat interconnected) aspects are reviewed in the first half of the book. Part A provides an introduction to pharmacology for the safety of drugs, an insightful guide that describes why/when/how to screen for off-target activities, and a discussion on important antitargets, like kinases and cardiac ion channels. Part B highlights four disease areas: psychiatric, cancer, bacterial infections, and epilepsy, and how polypharmacological drug discovery can fill the gap where conventional approaches are failing. Part C covers unique starting points for multi-targeted drug discovery programs and concludes with a discussion on multi-component therapeutics. Part D is a collection of various instructive case studies dedicated to the discovery of polypharmacological drugs, ranging from the anti-cancer drug sunitinib to the dual-acting drug candidate licofelone. The final chapter of the book illustrates the potential of target discovers, drug re-purposing, and the discovery of new drugs based on polypharmacology of existing pharmaceuticals. This book is a practical guide to help readers successfully navigate around the problems involved with promiscuous ligands and targets. It provides inspiration for new polypharmacological drug discovery projects with case studies, real examples, in-depth explanations and discussions, and detailed reviews and opinions on the topic.
