2011-04-20
Environmental and Genetic Factors Affecting Transport of Imatinib by OATP1A2
Publication
Publication
Clinical Pharmacology and Therapeutics , Volume 89 - Issue 6 p. 816- 820
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.
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| doi.org/10.1038/clpt.2011.42, hdl.handle.net/1765/26309 | |
| Clinical Pharmacology and Therapeutics | |
| Organisation | Erasmus MC: University Medical Center Rotterdam |
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Eechoute, K., Franke, R., Loos, W., Scherkenbach, L. A., de Boer, I., Verweij, J., … Sparreboom, A. (2011). Environmental and Genetic Factors Affecting Transport of Imatinib by OATP1A2. Clinical Pharmacology and Therapeutics, 89(6), 816–820. doi:10.1038/clpt.2011.42 |
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