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

Nicola F. Smith, William D. Figg, Alex Sparreboom*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

133 Scopus citations


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.

Original languageEnglish
Pages (from-to)429-445
Number of pages17
JournalExpert Opinion on Drug Metabolism and Toxicology
Issue number3
StatePublished - Oct 2005
Externally publishedYes


  • OATP
  • drug interaction
  • hepatic transport
  • pharmacogenetics


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