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Regorafenib and Zykadia

Determining the interaction of Regorafenib and Zykadia and the possibility of their joint administration.

Check result:
Regorafenib <> Zykadia
Relevance: 17.08.2022 Reviewer: Shkutko P.M., M.D., in

In the database of official manuals used in the service creation an interaction registered by statistical results of studies was found, which can either lead to negative consequences for the patient health or strengthen a mutual positive effect. A doctor should be consulted to address the issue of joint drug administration.

Consumer:

Consumer information for this interaction is not currently available.GENERALLY AVOID: Coadministration with potent inhibitors of CYP450 3A4 may increase the plasma concentrations of regorafenib and decrease the plasma concentrations of its active metabolites. In 18 healthy male study subjects, administration of a single 160 mg dose of regorafenib on day 5 of treatment with the potent CYP450 3A4 inhibitor ketoconazole (400 mg daily for 18 days) resulted in a 33% increase in mean regorafenib systemic exposure (AUC) compared to administration of regorafenib alone. Additionally, there was a 93% decrease each in the mean AUC of the M-2 and M-5 metabolites. Both have been shown to have similar in vitro pharmacological activity and steady-state concentrations as regorafenib, thus the net clinical effect of these pharmacokinetic changes is unknown. MANAGEMENT: Concomitant use of regorafenib with potent CYP450 3A4 inhibitors should generally be avoided. References "Product Information. Stivarga (regorafenib)." Bayer Pharmaceutical Inc, West Haven, CT.

Professional:

GENERALLY AVOID: Coadministration with potent inhibitors of CYP450 3A4 may increase the plasma concentrations of regorafenib and decrease the plasma concentrations of its active metabolites. In 18 healthy male study subjects, administration of a single 160 mg dose of regorafenib on day 5 of treatment with the potent CYP450 3A4 inhibitor ketoconazole (400 mg daily for 18 days) resulted in a 33% increase in mean regorafenib systemic exposure (AUC) compared to administration of regorafenib alone. Additionally, there was a 93% decrease each in the mean AUC of the M-2 and M-5 metabolites. Both have been shown to have similar in vitro pharmacological activity and steady-state concentrations as regorafenib, thus the net clinical effect of these pharmacokinetic changes is unknown.

MANAGEMENT: Concomitant use of regorafenib with potent CYP450 3A4 inhibitors should generally be avoided.

References
  • "Product Information. Stivarga (regorafenib)." Bayer Pharmaceutical Inc, West Haven, CT.
Regorafenib

Generic Name: regorafenib

Brand name: Stivarga

Synonyms: n.a.

Zykadia

Generic Name: ceritinib

Brand name: Zykadia

Synonyms: n.a.

In the course of checking the drug compatibility and interactions, data from the following reference sources was used: Drugs.com, Rxlist.com, Webmd.com, Medscape.com.

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