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The contributions by the leaders in the field of drug transport to the 1st and the 2nd editions of Drug Transporters have helped to secure a special role for this book in the education of students, fellows, and industrial practitioners in the pharmaceutical and biomedical sciences. The 2nd edition was published 8 years ago. Since then, there has been significant advances in the field including in‐depth understanding of membrane transporters in pediatric pharmacotherapy, new insights into the impact of these transporters on drug efficacy/safety, development of more sophisticated model systems and sensitive assay methods for studying drug transport in vitro and in vivo, and knowledge of transporters as drug targets for diseases. Therefore, it has become clear that a 3rd edition that serves to capture current advances in the field is both timely and necessary.

The new (3rd) edition will preserve the same basic format as that of the previous two editions: the first half of the book provides an overview of the relevant drug transporters useful for both beginning and experienced scientists and researchers. The second half of the book presents the principles of drug transport and associated techniques in sufficient detail to enable nonspecialist readers to understand them. Such readers include graduate students in the pharmacological or physiological sciences and academic or industrial scientists in related fields of study. There are 25 chapters in the 3rd edition as compared with 23 chapters in the 2nd edition. This represents an update of most of the chapters, significant expansion of others, removal of chapters for which content has been incorporated into other chapters, and addition of four new chapters. New chapters include in vitro–in vivo scale‐up of drug transport activities, application of physiologically based pharmacokinetic and pharmacodynamic modeling to delineating the role of various factors in drug disposition and toxicity, the ontogeny of drug transporters, and transporters as therapeutic targets for diseases. As a result, the new edition not only reflects where the field is today but where it will be for the foreseeable future. Like its predecessor, it is anticipated that the new edition will continue to be used as a textbook in graduate courses in Drug/Membrane Transport and as a desk reference for researchers working in the transporter field, as well as in the areas of drug metabolism and pharmacokinetics/pharmacodynamics in the pharmaceutical industry.

We would like to express our deepest gratitude and respect to our colleagues who contributed chapters in their area of expertise. The book was written and edited during an especially difficult and challenging time of global pandemic, with many of our colleagues being affected both professionally and personally. We are indebted to all of our contributors. We acknowledge the many professionals at John Wiley & Sons, Inc. who worked with us to ensure the best book possible. On a personal note, we thank our families for their love and support.

Guofeng You and Marilyn E. Morris