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  • Title: Effect of rifampin on the pharmacokinetics of Axitinib (AG-013736) in Japanese and Caucasian healthy volunteers.
    Author: Pithavala YK, Tortorici M, Toh M, Garrett M, Hee B, Kuruganti U, Ni G, Klamerus KJ.
    Journal: Cancer Chemother Pharmacol; 2010 Feb; 65(3):563-70. PubMed ID: 19603168.
    Abstract:
    PURPOSE: Axitinib, a potent and selective inhibitor of vascular endothelial growth factor receptors 1, 2, 3, is metabolized by cytochrome P450 3A4 and glucuronidation. This study evaluated the effect of rifampin, a potent inducer of drug-metabolizing enzymes, on axitinib plasma pharmacokinetics. Equal numbers of Japanese and Caucasian subjects were enrolled to assess the potential differences in axitinib pharmacokinetics between the two ethnicities. METHODS: Forty healthy volunteers were randomized to receive 5 mg axitinib alone and with 600 mg rifampin. RESULTS: Rifampin expectedly decreased AUCinf and Cmax of axitinib (geometric mean reduced by 79 and 71%, respectively). However, differences in axitinib pharmacokinetics were not observed between Japanese and Caucasian subjects (geometric mean ratios for axitinib treatment alone for AUCinf and Cmax were 103 and 96%). CONCLUSIONS: The results support a common axitinib starting dose in both populations. Potent inducers of drug-metabolizing enzymes reduce axitinib exposure and dose adjustments may be needed for optimal efficacy.
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