Environmental and genetic factors affecting transport of imatinib by OATP1A2

K. Eechoute, R. M. Franke, W. J. Loos, L. A. Scherkenbach, I. Boere, J. Verweij, H. Gurney, R. B. Kim, R. G. Tirona, R. H.J. Mathijssen, A. Sparreboom

Research output: Contribution to journalArticlepeer-review

50 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)816-820
Number of pages5
JournalClinical Pharmacology and Therapeutics
Issue number6
Publication statusPublished - 2011
Externally publishedYes


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