Relevance of Transporters in Clinical Studies

  • Bruno HagenbuchEmail author
Living reference work entry


It has become clear that drug disposition is not just a result of passive diffusion and metabolizing enzymes. Numerous transporters were identified in recent years to be involved in the absorption, distribution, and excretion of essentially all drugs. While transporters of the solute carrier (SLC) family are mainly involved in the uptake of drugs into cells, ATP-binding cassette (ABC) transporters are responsible for their efflux. Among the more than 420 SLC and 47 ABC transporters, only about 25 seem to be important for the disposition of over-the-counter and prescription drugs. Among these the Food and Drug Administration (FDA), the European Medicines Agency (EMA), and the Japanese Pharmaceuticals and Medical Devices Agency (PMDA) have identified seven transporters which need to be tested for investigational drugs and an additional five transporters that are considered to be important. Two of the seven transporters, the multidrug resistance protein 1 (MDR1) and the breast cancer resistance protein (BCRP), are ABC transporters. The other five, the organic cation transporter 2 (OCT2), the organic anion transporter 1 (OAT1) and 3 (OAT3), and the organic anion transporting polypeptide 1B1 (OATP1B1) and 1B3 (OATP1B3), are SLC transporters. If additional transporters become clinically relevant, they may be added by the regulatory agencies to the list or required transporters.



The author would like to acknowledge the National Institutes of Health grant GM077336.

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Copyright information

© Springer International Publishing AG, part of Springer Nature 2018

Authors and Affiliations

  1. 1.Department of Pharmacology, Toxicology and TherapeuticsThe University of Kansas Medical CenterKansas CityUSA

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