Transporters in Drug Discovery and Development: Detailed Concepts and Best Practice, 2nd Edition is a comprehensive book providing a detailed overview of significant drug transporter families, their roles in disease causation due to functional defects, and their importance in drug discovery and development. Building upon the foundation set by the first edition, this updated version covers various topics, including clinically relevant drug transporter-related pharmacokinetics variations, drug-drug interactions (DDIs), genetic polymorphisms, transporter-related organ toxicity, and methodologies for studying drug transporters. It also highlights the translational aspect in drug discovery and development. The revision explores the advancements in transporter research, such as the emerging use of transporters as pharmacological targets, the evolving application of modeling and simulation, and the innovative use of endogenous biomarkers in assessing transporter activities during drug clinical trials. Transporters in Drug Discovery and Development: Detailed Concepts and Best Practice, 2nd Edition provides a deeper understanding of transporter research and its implications. It is an invaluable resource for researchers, students, and professionals in the field, offering insights that could potentially revolutionize drug discovery and development.