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A strong CYP3A4/P-gp inhibitor (ketoconazole) increased the systemic exposure of ceritinib, which may increase the incidence and severity of adverse reactions of Ceritinib. Avoid concurrent use of strong CYP3A inhibitors during treatment with Ceritinib. If concurrent use of strong CYP3A inhibitors is unavoidable, reduce the Ceritinib dose. Do not consume grapefruit and grapefruit juice as they may inhibit CYP3A.
A strong CYP3A4/P-gp inducer (rifampin) decreased the systemic exposure of ceritinib, which may decrease the efficacy of Ceritinib. Avoid concurrent use of strong CYP3A inducers during treatment with Ceritinib.
CYP3A Substrates Ceritinib increased the systemic exposure of a sensitive CYP3A substrate (midazolam). Avoid coadministration of Ceritinib with sensitive CYP3A substrates. If concomitant use is unavoidable, consider dose reduction of the sensitive CYP3A substrate(s). If Ceritinib is coadministered with other CYP3A substrates, refer to the CYP3A substrate labeling for dosage recommendation with strong CYP3A inhibitors.
Ceritinib increased the systemic exposure of a CYP2C9 substrate (warfarin). Increase the frequency of INR monitoring if coadministration with warfarin is unavoidable as the anti-coagulant effect of warfarin may be enhanced.
Avoid coadministration of Ceritinib with CYP2C9 substrates for which minimal concentration changes may lead to serious toxicities. If concomitant use of such CYP2C9 substrates is unavoidable, consider dose reduction for the coadministered CYP2C9 substrates.
Ceritinib causes concentration-dependent increases in the QTc interval. When possible, avoid coadministration of Ceritinib with other products with a known potential to prolong the QTc interval.
Ceritinib can cause bradycardia. When possible, avoid coadministration of Ceritinib with other products known to cause bradycardia.
from FDA，2021.10
