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 journalArticleResearchpeer-review

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.

LanguageEnglish
Pages816-820
Number of pages5
JournalClinical Pharmacology and Therapeutics
Volume89
Issue number6
DOIs
Publication statusPublished - 2011
Externally publishedYes

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Drug Interactions
Duodenum
Biological Availability
Anions
Peptides
Pharmaceutical Preparations
Imatinib Mesylate
Neoplasms
In Vitro Techniques
Rosuvastatin Calcium

Cite this

Eechoute, K., Franke, R. M., Loos, W. J., Scherkenbach, L. A., Boere, I., Verweij, J., ... Sparreboom, A. (2011). Environmental and genetic factors affecting transport of imatinib by OATP1A2. Clinical Pharmacology and Therapeutics, 89(6), 816-820. https://doi.org/10.1038/clpt.2011.42
Eechoute, K. ; Franke, R. M. ; Loos, W. J. ; Scherkenbach, L. A. ; Boere, I. ; Verweij, J. ; Gurney, H. ; Kim, R. B. ; Tirona, R. G. ; Mathijssen, R. H.J. ; Sparreboom, A. / Environmental and genetic factors affecting transport of imatinib by OATP1A2. In: Clinical Pharmacology and Therapeutics. 2011 ; Vol. 89, No. 6. pp. 816-820.
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Eechoute, K, Franke, RM, Loos, WJ, Scherkenbach, LA, Boere, I, Verweij, J, Gurney, H, Kim, RB, Tirona, RG, Mathijssen, RHJ & Sparreboom, A 2011, 'Environmental and genetic factors affecting transport of imatinib by OATP1A2', Clinical Pharmacology and Therapeutics, vol. 89, no. 6, pp. 816-820. https://doi.org/10.1038/clpt.2011.42

Environmental and genetic factors affecting transport of imatinib by OATP1A2. / Eechoute, K.; Franke, R. M.; Loos, W. J.; Scherkenbach, L. A.; Boere, I.; Verweij, J.; Gurney, H.; Kim, R. B.; Tirona, R. G.; Mathijssen, R. H.J.; Sparreboom, A.

In: Clinical Pharmacology and Therapeutics, Vol. 89, No. 6, 2011, p. 816-820.

Research output: Contribution to journalArticleResearchpeer-review

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