Pharmacological and Toxicological Significance of the Organic Cation Transporters OCT and MATE: Drug Disposition, Interaction and Toxicity

  • Hideyuki MotohashiEmail author
  • Ken-ichi Inui


Organic cation transporter OCTs and multidrug and toxin extrusion (MATE) are involved in pharmacokinetics of various drugs. In the renal proximal epithelia, OCT2 mediates uptake of the drugs such as metformin or cimetidine at basolateral membrane, and MATE1 and MATE2-K mediated the secretion of cationic and zwitterionic drugs at brush-border membrane. In the liver, OCT1 are expressed on the sinusoidal membrane and MATE1 are expressed on the canalicular membrane. These transporters mediate the biliary excretion of drugs. The change of these transporter activities, caused by genetic alteration or drug–drug interaction, affected the pharmacokinetics of substrates. Inhibitors of the transporters reduce the biliary or urinary secretion of substrate drugs. In addition, OCTs and MATEs are involved in adverse drug reactions. For example, it was considered that renal toxicities of platinum agents cisplatine or oxaliplatin were affected by substrate specificities of renal OCT2 and MATEs. OCTs and MATEs play important roles for drug efficacies and toxicities especially in the liver and the kidney.


Drug–drug interaction Kidney Liver Renal secretion Renal toxicity Platinum agents 


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© Springer International Publishing Switzerland 2016

Authors and Affiliations

  1. 1.Kyoto Pharmaceutical UniversityYamashina-kuJapan

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