Environmental and genetic factors affecting transport of imatinib by OATP1A2

Clin Pharmacol Ther. 2011 Jun;89(6):816-20. doi: 10.1038/clpt.2011.42. Epub 2011 Apr 20.


The bioavailability of orally administered imatinib is >90%, although the drug is monocationic under the acidic conditions in the duodenum. In vitro, we found that imatinib is transported by the intestinal uptake carrier organic anion transporting polypeptide (OATP1A2) and that this process is sensitive to pH, rosuvastatin, and genetic variants. However, in a study in patients with cancer, imatinib absorption was not associated with OATP1A2 variants and was unaffected by rosuvastatin. These findings highlight the importance of verifying in a clinical setting the drug-transporter interactions observed in in vitro tests.

Publication types

  • Comparative Study
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzamides
  • Biological Transport, Active / physiology
  • Environment*
  • Female
  • HeLa Cells
  • Humans
  • Imatinib Mesylate
  • Organic Anion Transporters / genetics*
  • Organic Anion Transporters / metabolism*
  • Piperazines / antagonists & inhibitors
  • Piperazines / metabolism*
  • Pyrimidines / antagonists & inhibitors
  • Pyrimidines / metabolism*
  • Xenopus laevis


  • Benzamides
  • Organic Anion Transporters
  • Piperazines
  • Pyrimidines
  • SLCO1A2 protein, human
  • Imatinib Mesylate