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In vitro evidence showed that the drug is metabolized through cytochrome P450 (CYP) 3A4 and aldoketoreductases and does not inhibit any of the major CYP isoenzymes. In a clinical pharmacokinetic study, the specific inhibition of CYP3A4 by ketoconazole showed no significant effects on the pharmacokinetics of exemestane.
Although pharmacokinetic effects were observed in a pharmacokinetic interaction study with rifampicin, a potent CYP3A4 inducer, the pharmacologic activity (i.e., estrogen suppression) was not affected, and a dosage adjustment is not required.
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