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Article

Gemfibrozil impairs imatinib absorption and inhibits the CYP2C8-mediated formation of its main metabolite.

Clinical pharmacology and therapeutics - 1 Sept 2013

Filppula A M, Tornio A, Niemi M, Neuvonen P J, Backman J T

Abstract excerpt

Cytochrome P450 (CYP) 3A4 is considered the most important enzyme in imatinib biotransformation. In a randomized, crossover study, 10 healthy subjects were administered gemfibrozil 600 mg or placebo twice daily for 6 days, and imatinib 200 mg on day 3, to study the significance of CYP2C8 in imatinib pharmacokinetics. Unexpectedly, gemfibrozil reduced the peak plasma concentration (Cmax) of imatinib by 35% (P <...

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PMID: 23657159
DOI: 10.1038/clpt.2013.92

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