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Since the discovery of transporter‐mediated drug transport, and the subsequent cloning and functional characterization of the individual transporter, our understanding of the roles of drug transporters play in human physiology, diseases, and drug therapy has exploded. Information about any of the many diverse aspects of drug transporters is scattered very widely, from journals of microbiology to those of pharmacology and genetics. Furthermore, many different, often conflicting, explanations given for these transporters need to be reconciled and rationalized. With such a need, comes this book Drug Transporters. This book, now in its 3rd edition, compiles and synthesizes the diverse body of knowledge on currently known drug transporters. This chapter provides an overview on the basic concepts/properties of drug transporters to serve as a foundation, allowing readers the opportunity to become familiar with those notions prior to reading the following chapters in the entire book.