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Expert Opin Drug Metab Toxicol. 2005 Oct;1(3):429-45.

Role of the liver-specific transporters OATP1B1 and OATP1B3 in governing drug elimination.

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National Cancer Institute, Molecular Pharmacology Section, Medical Oncology Branch, Center for Cancer Research, 9000 Rockville Pike, Bethesda, MD 20892, USA.


Members of the organic anion transporting polypeptide (OATP) family are responsible for the cellular uptake of a broad range of endogenous compounds and xenobiotics in multiple tissues. This review focuses on OATP1B1 and -1B3, which are specifically expressed in the liver and considered to be of particular importance for hepatic drug elimination and drug pharmacokinetics. Recent literature has indicated that inhibition of these transporters may result in drug-drug interactions. Furthermore, genetic polymorphisms in the genes encoding OATP1B1 and -1B3 have been described that increase or decrease transport in vitro and in vivo. Alteration of transporter function by either of these mechanisms may contribute to interindividual variability in drug disposition and response. In this review an update of this rapidly emerging field is provided.

[Indexed for MEDLINE]

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