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

doi:10.1038/clpt.2011.42

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

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Abstract

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 language	English
Pages (from-to)	816-820
Number of pages	5
Journal	Clinical Pharmacology & Therapeutics
Volume	89
Issue number	6
DOIs	https://doi.org/10.1038/clpt.2011.42
Publication status	Published - Jun 2011

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abstract = "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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AU - Eechoute, K.

AU - Franke, R. M.

AU - Loos, W. J.

AU - Scherkenbach, L. A.

AU - Boere, I.

AU - Verweij, J.

AU - Gurney, H.

AU - Kim, R. B.

AU - Tirona, R. G.

AU - Mathijssen, R. H.J.

AU - Sparreboom, A.

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JO - Clinical Pharmacology & Therapeutics

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Environmental and genetic factors affecting transport of imatinib by OATP1A2

Abstract

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