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Bosutinib and Zykadia

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

Check result:
Bosutinib <> Zykadia
Relevance: 06.06.2022 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 and moderate inhibitors of CYP450 3A4 may significantly increase the plasma concentrations of bosutinib, which is primarily metabolized by the isoenzyme. In 24 healthy volunteers, administration of a single 100 mg dose of bosutinib with the potent CYP450 3A4 inhibitor ketoconazole (400 mg/day for 5 days) under fasting conditions resulted in a 5.2-fold increase in bosutinib peak plasma concentration (Cmax) and 8.6-fold increase in systemic exposure (AUC) compared to administration of bosutinib alone. Ketoconazole also decreased the mean apparent clearance of bosutinib by approximately 9-fold and increased the mean terminal half-life from 46.2 hours to 69.0 hours. MANAGEMENT: Concomitant use of bosutinib with potent or moderate CYP450 3A4 inhibitors should generally be avoided. If use of a potent or moderate CYP450 3A4 inhibitor is required, an interruption or a dosage reduction of bosutinib therapy should be considered. References Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0 "Product Information. Bosulif (bosutinib)." Pfizer U.S. Pharmaceuticals Group, New York, NY.

Professional:

GENERALLY AVOID: Coadministration with potent and moderate inhibitors of CYP450 3A4 may significantly increase the plasma concentrations of bosutinib, which is primarily metabolized by the isoenzyme. In 24 healthy volunteers, administration of a single 100 mg dose of bosutinib with the potent CYP450 3A4 inhibitor ketoconazole (400 mg/day for 5 days) under fasting conditions resulted in a 5.2-fold increase in bosutinib peak plasma concentration (Cmax) and 8.6-fold increase in systemic exposure (AUC) compared to administration of bosutinib alone. Ketoconazole also decreased the mean apparent clearance of bosutinib by approximately 9-fold and increased the mean terminal half-life from 46.2 hours to 69.0 hours.

MANAGEMENT: Concomitant use of bosutinib with potent or moderate CYP450 3A4 inhibitors should generally be avoided. If use of a potent or moderate CYP450 3A4 inhibitor is required, an interruption or a dosage reduction of bosutinib therapy should be considered.

References
  • Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
  • "Product Information. Bosulif (bosutinib)." Pfizer U.S. Pharmaceuticals Group, New York, NY.
Bosutinib

Generic Name: bosutinib

Brand name: Bosulif

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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