Importance of drug transporters in pharmacokinetics and drug safety

The exact role of transporters in the absorption, distribution, and excretion (ADE) of drugs is still being elucidated; however, current evidence suggests that their role in these processes may be significant. In this review, the role of transporters in the ADE, pharmacology, toxicology, and clinical drug-drug interactions (DDIs) of drugs will be discussed. The current biological tools to assess this role and practical perspectives for the utilization of knowledge about drug transporters to drug discovery and development will also be discussed. Currently, regulatory agencies are focusing on these potential transporter-mediated DDIs. Therefore, guidance and caution on the investigation of these DDIs will be given.