Drug Interactions between Bosulif and repotrectinib
This report displays the potential drug interactions for the following 2 drugs:
- Bosulif (bosutinib)
- repotrectinib
Interactions between your drugs
bosutinib repotrectinib
Applies to: Bosulif (bosutinib) and repotrectinib
Consumer information for this interaction is not currently available.
GENERALLY AVOID: Coadministration with potent and moderate inducers of CYP450 3A4 may significantly decrease the plasma concentrations of bosutinib, which is primarily metabolized by the isoenzyme. In 24 healthy volunteers, administration of a single 500 mg dose of bosutinib with the potent CYP450 3A4 inducer rifampin (600 mg/day for 6 days) under fed conditions resulted in an 86% decrease in bosutinib peak plasma concentration (Cmax) and 94% decrease in systemic exposure (AUC) compared to administration of bosutinib alone.
MANAGEMENT: Concomitant use of bosutinib with potent and moderate CYP450 3A4 inducers should be avoided due to the potential for reduced efficacy.
References
- "Product Information. Bosulif (bosutinib)." Pfizer U.S. Pharmaceuticals Group (2012):
Drug and food interactions
repotrectinib food
Applies to: repotrectinib
Consumer information for this interaction is not currently available.
GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations and adverse effects of repotrectinib. According to prescribing information, repotrectinib is primarily metabolized by CYP450 3A4, and is also a substrate of P-gp in vitro. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. Inhibition of hepatic CYP450 3A4 may also contribute. The interaction has not been studied with repotrectinib and grapefruit juice but has been reported for other CYP450 3A4 inhibitors. Drug interaction studies have shown that the administration of repotrectinib with itraconazole, a potent CYP450 3A4 and P-gp inhibitor, increased the peak plasma concentration (Cmax) and systemic exposure (AUC) of repotrectinib by 1.7-fold and 5.9-fold, respectively. In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands. Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition. Increased exposure to repotrectinib may increase the risk of adverse reactions such as dizziness, fatigue, cognitive disorders, ataxia, dysgeusia, peripheral neuropathy, muscular weakness, and dyspnea as well as more serious adverse effects such as interstitial lung disease/pneumonitis, liver transaminase elevations, myalgia with creatinine phosphokinase (CPK) elevation, hyperuricemia, and skeletal fractures.
MANAGEMENT: The manufacturer advises that concomitant use of repotrectinib with grapefruit, grapefruit juice, or supplements that contain grapefruit should be avoided.
References
- "Product Information. Augtyro (repotrectinib)." Bristol-Myers Squibb ORIG-1 (2023):
bosutinib food
Applies to: Bosulif (bosutinib)
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.
Therapeutic duplication warnings
No warnings were found for your selected drugs.
Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.
See also
Drug Interaction Classification
Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit. | |
Moderately clinically significant. Usually avoid combinations; use it only under special circumstances. | |
Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan. | |
No interaction information available. |
Further information
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
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