The organic anion-transporting polypeptides (OATP) represent a family of proteins responsible for the membrane transport of a large number of endogenous and xenobiotic compounds with diverse chemical characteristics. OATPs are expressed in liver, kidney, brain and intestine suggesting that they may play a critical role in drug disposition. Naturally occurring polymorphisms in OATPs are currently being identified and for some, in vitro transport activities have been characterized. In this article, we review the molecular, biochemical and pharmacological aspects of known human OATPs including the presence and functional relevance of genetic polymorphisms.