Pharmacogenetics of membrane transporters: An update on current approaches

Tristan M. Sissung, Caitlin E. Baum, C. Tyler Kirkland, Rui Gao, Erin R. Gardner, William D. Figg

Research output: Contribution to journalReview articlepeer-review

104 Scopus citations


This review provides an overview of the pharmacogenetics of membrane transporters including selected ABC transporters (ABCB1, ABCC1, ABCC2, and ABCG2) and OATPs (OATP1B1 and OATP1B3). Membrane transporters are heavily involved in drug clearance and alters drug disposition by actively transporting substrate drugs between organs and tissues. As such, polymorphisms in the genes encoding these proteins may have significant effects on the absorption, distribution, metabolism and excretion of compounds, and may alter pharmacodynamics of many agents. This review discusses the techniques used to identify substrates and inhibitors of these proteins and subsequently to assess the effect of genetic mutation on transport, both in vitro and in vivo. A comprehensive list of substrates for the major drug transporters is included. Finally, studies linking transporter genotype with clinical outcomes are discussed.

Original languageEnglish
Pages (from-to)152-167
Number of pages16
JournalMolecular Biotechnology
Issue number2
StatePublished - Feb 2010
Externally publishedYes


  • ABCB1
  • ABCC1
  • ABCC2
  • ABCG2
  • Membrane transporters
  • OATP1B1
  • OATP1B3
  • Pharmacogenetics


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