Summary: - a comprehensive overview of drug transporter families and their clinical relevance in drug discovery and development - balanced coverage of molecular biology aspects and functional outcomes - state of art knowledge related to transporter mediated DDI and the clinical relevance in pharmacokinetics, dynamics and toxicity - clinical implications of drug transporters in genetic polymorphism and inter-subject/ethnic group variance - highly practical: provides sufficient details to enable the scientists working in biopharmaceutical science, drug discovery/development in understanding the principles and techniques for testing drug candidates. Decision trees to guide clinical studies of drug transporter interactions are proposed and described Written by a leading researcher in the field, Transporters in drug discovery and development provides a comprehensive and practical guide to drug transporter families that are the most important for drug discovery and development. It covers: an overview of transporter families and organ distribution; clinical relevant drug-drug interaction; clinical relevant polymorphism; drug transporter related pharmacokinetic, pharmacodynamics and toxicity; in vitro/in vivo probes of drug transport studies; the practical methodologies of industrial transporter screening and translational aspect in drug discovery and developments. About the Author: Yurong Lai is a senior principal scientist at a US-based pharmaceutical company. He received his M.D. from Fujian Medical University in China and a Ph.D.

(Toxicology) from Sapporo Medical University in Japan. From 1998 to 2001, he was a research fellow of Japanese Society for Promotion (JSPS) in Department of Physiopathology, Graduate School of Medicine of Hokkaido University, followed by a position as Research Associate in Department of Pharmaceutics, University of Washington. Contents: Membrane transporters and the diseases corresponding to functional defects; P-glycoprotein (P-gp/MDR1)/ABCB1; Multidrug resistance- associated protein 2 (MRP2/ABCC2); Breast cancer resistance protein (BCRP)/ABCG2; The bile salt export pump (BSEP/ABCB11); Organic anion- transporting polypeptides (OATPs/SLCOs); Organic anion, organic cation and zwitterion transporters of the SLC22 and SLC47 superfamily (OATs, OCTs, OCTNs and MATEs); Drug transporters in drug discovery and development; Transporter study methodologies.