CYP3A4 Inducers
Administration of rifampin (600 mg for 9 days), a strong CYP3A4 inducer, with a single dose of
regorafenib (160 mg on day 7) resulted in a reduction in mean regorafenib exposure (AUC) of
approximately 50%, a 3- to 4-fold increase in mean exposure of the active metabolite M-5, and
no change in exposure of active metabolite M-2. Other strong inducers of CYP3A4 activity
(eg, phenytoin, carbamazepine phenobarbital and St. John’s Wort) may also increase metabolism
of regorafenib. Avoid concomitant administration of regorafenib with strong CYP3A4 inducers.
CYP3A4 InducersAdministration of rifampin (600 mg for 9 days), a strong CYP3A4 inducer, with a single dose ofregorafenib (160 mg on day 7) resulted in a reduction in mean regorafenib exposure (AUC) ofapproximately 50%, a 3- to 4-fold increase in mean exposure of the active metabolite M-5, andno change in exposure of active metabolite M-2. Other strong inducers of CYP3A4 activity(eg, phenytoin, carbamazepine phenobarbital and St. John’s Wort) may also increase metabolismof regorafenib. Avoid concomitant administration of regorafenib with strong CYP3A4 inducers.
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