The past few years have ushered in a wealth of new information on transporter biology, ranging from the publication of new crystal structures of the human glucose transporters (SLC2A2)1 to the discovery of the mechanism by which the monocarboxylate transporter (SLC16A11) associates with type 2 diabetes,2 to a plethora of new therapies that target transporters in the treatment of both common and rare diseases. Complementing these fundamental advances in transporter biology, great strides have been made in our understanding of the role of transporters in the pharmacokinetics and pharmacodynamics of drugs, including transporter‐mediated drug–drug interactions (DDIs), nutrient–drug interactions, and drug efficacy and safety.3-5 The International Transporter Consortium (ITC) sponsored its third workshop as a preconference to the Annual Meeting of the American Society for Clinical Pharmacology and Therapeutics in the spring of 2017. The major goal of the preconference was to summarize recent advances in transporter pharmacology, which are of particular relevance to the development, approval, and safe and effective use of prescription drugs. A range of topics, including computational modeling of drug–transporter interactions and emerging transporters of clinical importance, were presented, culminating in 10 articles that are featured in this issue of Clinical Pharmacology & Therapeutics. These articles summarize recent advances in transporters in drug development and include a summary of a wealth of new information and a review of the recent relevant literature.