Drug Transporters

Volume 201 of the series Handbook of Experimental Pharmacology pp 105-167


Organic Cation Transporters (OCTs, MATEs), In Vitro and In Vivo Evidence for the Importance in Drug Therapy

  • Anne T. NiesAffiliated withDr. Margarete Fischer-Bosch Institute of Clinical PharmacologyUniversity of Tübingen Email author 
  • , Hermann KoepsellAffiliated withInstitute of Anatomy and Cell Biology, University of Würzburg
  • , Katja DammeAffiliated withDr. Margarete Fischer-Bosch Institute of Clinical PharmacologyUniversity of Tübingen
  • , Matthias SchwabAffiliated withDr. Margarete Fischer-Bosch Institute of Clinical PharmacologyDepartment of Clinical Pharmacology, University Hospital Tübingen

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Organic cation transporters (OCTs) of the solute carrier family (SLC) 22 and multidrug and toxin extrusion (MATE) transporters of the SLC47 family have been identified as uptake and efflux transporters, respectively, for xenobiotics including several clinically used drugs such as the antidiabetic agent metformin, the antiviral agent lamivudine, and the anticancer drug oxaliplatin. Expression of human OCT1 (SLC22A1) and OCT2 (SLC22A2) is highly restricted to the liver and kidney, respectively. By contrast, OCT3 (SLC22A3) is more widely distributed. MATEs (SLC47A1, SLC47A2) are predominantly expressed in human kidney. Data on in vitro studies reporting a large number of substrates and inhibitors of OCTs and MATEs are systematically summarized. Several genetic variants of human OCTs and in part of MATE1 have been reported, and some of them result in reduced in vitro transport activity corroborating data from studies with knockout mice. A comprehensive overview is given on currently known genotype–phenotype correlations for variants in OCTs and MATE1 related to protein expression, pharmacokinetics/-dynamics of transporter substrates, treatment outcome, and disease susceptibility.


Drug transporters Organic cation transport Excretion OCT1 OCT2 OCT3 MATE1 MATE2-K Liver Kidney tissue distribution Knockout mice Pharmacogenomics Genotype–phenotype correlation Metformin Single nucleotide polymorphisms Drug response Interindividual variability Drug–drug interaction Pharmacokinetics