Role of organic cation transporters in the renal handling of therapeutic agents and xenobiotics

Toxicol Appl Pharmacol. 2005 May 1;204(3):309-19. doi: 10.1016/j.taap.2004.10.021.


Organic cations (OCs) constitute a diverse array of compounds of physiological, pharmacological, and toxicological importance. Renal secretion of these compounds, which occurs principally along the proximal portion of the nephron, plays a critical role in regulating the concentration of OCs in the plasma and in clearing the body of potentially toxic xenobiotic OCs. Transepithelial OC transport in the kidney involves separate entry and exit steps at the basolateral and luminal aspects of renal tubular cells. It is increasingly apparent that basolateral and luminal OC transport reflects the concerted activity of a suite of separate transport processes arranged in parallel in each pole of proximal tubule cells. Most of the transporters that appear to dominate renal secretion of OCs belong to a single family of transport proteins: the OCT Family. The characterization of their activity, and their localization within distinct regions of the kidney, has permitted development of models describing the molecular and cellular basis of the renal secretion of OCs.

Publication types

  • Review

MeSH terms

  • Animals
  • Humans
  • Kidney / metabolism*
  • Organic Cation Transport Proteins / genetics
  • Organic Cation Transport Proteins / metabolism*
  • Organic Cation Transport Proteins / physiology
  • Pharmaceutical Preparations / metabolism*
  • Xenobiotics / metabolism*


  • Organic Cation Transport Proteins
  • Pharmaceutical Preparations
  • Xenobiotics