Abstract

Drug transporters are widely expressed in organs and tissue barriers throughout human and animal bodies. Studies over the last two decades have identified various ATP-binding cassette and solute carrier transporters that play critical roles in the absorption, distribution, metabolism, and elimination of drugs and xenobiotics. This special section contains more than 20 original manuscripts and reviews that cover the most recent advances in the areas of drug transporter research, including the basic biology and function of transporters, expression of drug transporters in organ and tissue barriers, the mechanisms underlying regulation of transporter expression, transporter-mediated drug disposition in animal models, and the development and utilization of new technologies in drug transporter study, as well as pharmacokinetic modeling and simulation to assess transporter involvement in drug disposition and drug-drug interactions. We believe that the topics covered in this special section will advance our understanding of the roles of transporters in drug disposition, efficacy, and safety.