Drug Interaction Report

Consumer information for this interaction is not currently available.

MONITOR: Coadministration with inhibitors of CYP450 3A4 and/or P-glycoprotein (P-gp) may increase the plasma concentrations of bosutinib, which is a substrate of the isoenzyme and efflux transporter. In 24 healthy volunteers, administration of a single 100 mg dose of bosutinib with the potent CYP450 3A4 and P-gp 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. No data are available for use with less potent CYP450 3A4 inhibitors or P-gp inhibitors.

MANAGEMENT: Caution is advised when bosutinib is used with CYP450 3A4 or P-gp inhibitors. Patients should be monitored more closely for development of adverse effects such as diarrhea, nausea, vomiting, abdominal pain, myelosuppression, hepatotoxicity, and fluid retention (e.g., pericardial effusion, pleural effusion, pulmonary edema, peripheral edema).

Bosutinib should be taken with a meal to help with its absorption. Do not consume grapefruit, grapefruit juice, or any supplements that contain grapefruit extract during treatment with bosutinib unless directed otherwise by your doctor. Grapefruit juice can significantly increase the blood levels of bosutinib. You may be more likely to experience side effects such as nausea, vomiting, abdominal pain, diarrhea, liver damage, and impaired bone marrow function resulting in low numbers of different types of blood cells, which can increase the risk of anemia, bleeding problems, and infections. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.