In vitro and in vivo evidence of the importance of organic anion transporters (OATs) in drug therapy

Handb Exp Pharmacol. 2011;(201):29-104. doi: 10.1007/978-3-642-14541-4_2.


Organic anion transporters 1-10 (OAT1-10) and the urate transporter 1 (URAT1) belong to the SLC22A gene family and accept a huge variety of chemically unrelated endogenous and exogenous organic anions including many frequently described drugs. OAT1 and OAT3 are located in the basolateral membrane of renal proximal tubule cells and are responsible for drug uptake from the blood into the cells. OAT4 in the apical membrane of human proximal tubule cells is related to drug exit into the lumen and to uptake of estrone sulfate and urate from the lumen into the cell. URAT1 is the major urate-absorbing transporter in the apical membrane and is a target for uricosuric drugs. OAT10, also located in the luminal membrane, transports nicotinate with high affinity and interacts with drugs. Major extrarenal locations of OATs include the blood-brain barrier for OAT3, the placenta for OAT4, the nasal epithelium for OAT6, and the liver for OAT2 and OAT7. For all transporters we provide information on cloning, tissue distribution, factors influencing OAT abundance, interaction with endogenous compounds and different drug classes, drug/drug interactions and, if known, single nucleotide polymorphisms.

Publication types

  • Review

MeSH terms

  • Age Factors
  • Animals
  • Biological Transport
  • Drug Interactions
  • Evidence-Based Medicine
  • Genotype
  • Humans
  • Kidney / metabolism
  • Organic Anion Transporters / drug effects
  • Organic Anion Transporters / genetics
  • Organic Anion Transporters / metabolism*
  • Pharmaceutical Preparations / metabolism*
  • Pharmacogenetics
  • Phenotype
  • Polymorphism, Single Nucleotide
  • Sex Factors
  • Species Specificity


  • Organic Anion Transporters
  • Pharmaceutical Preparations