The role of organic ion transporters in drug disposition: an update

Abstract

Transporters for organic anions and organic cations in kidney, liver, intestine, brain, and placenta play essential roles in drug disposition. The cloning and characterization of these transporters have significantly advanced our understanding of the molecular and cellular mechanisms of the drug disposition process. This review aims at updating the recent knowledge of general properties, structure-function relationships, and regulation mechanisms of the organic anion transporters (OATs) and the organic cation transporters (OCTs). Such information will be essential for the design and development of new drugs to maximize therapeutic efficacy and minimize drug-induced toxicity as well as unwanted drug-drug interactions.