Drug Interactions between berotralstat and Imbruvica
This report displays the potential drug interactions for the following 2 drugs:
- berotralstat
- Imbruvica (ibrutinib)
Interactions between your drugs
ibrutinib berotralstat
Applies to: Imbruvica (ibrutinib) and berotralstat
ADJUST DOSE: Coadministration with inhibitors of P-glycoprotein (P-gp) and/or breast cancer resistance protein (BCRP) may significantly increase the plasma concentrations of berotralstat. Berotralstat is a substrate of both P-gp and BCRP. Coadministration with potent P-gp and BCRP inhibitor cyclosporine increased berotralstat peak plasma concentration (Cmax) and total systemic drug exposure (AUC 0-inf) by 25% and 69%, respectively. Increased plasma concentrations of berotralstat may increase the risk of adverse effects, including the potential for QT prolongation. Berotralstat may cause concentration-dependent prolongation of the Fridericia-corrected QT interval (QTcF). A mean increase in the QTcF interval of 15.9 milliseconds has been reported at 3-times the recommended dose of berotralstat; however, berotralstat has not been shown to prolong the QT interval to any clinically relevant extent when administered at the recommended daily dose of 150 mg. Data are not available for other, less potent P-gp and/or BCRP inhibitors.
MANAGEMENT: The dosage of berotralstat should be reduced to 110 mg once daily in patients requiring chronic coadministration with P-gp and/or BCRP inhibitors. Patients should be advised to contact their physician if they experience undue adverse effects of berotralstat such as abdominal pain, vomiting, or diarrhea. Patients should seek prompt medical attention if they experience symptoms that could indicate the occurrence of torsade de pointes such as dizziness, lightheadedness, fainting, palpitations, irregular heartbeat, shortness of breath, or syncope.
References
- Cerner Multum, Inc. "UK Summary of Product Characteristics."
- (2021) "Product Information. Orladeyo (berotralstat)." BioCryst Pharmaceuticals Inc
Drug and food interactions
ibrutinib food
Applies to: Imbruvica (ibrutinib)
GENERALLY AVOID: Coadministration with grapefruit, grapefruit juice, or Seville oranges may significantly increase the plasma concentrations of ibrutinib. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. Pharmacokinetic modeling suggests that other moderate CYP450 3A4 inhibitors such as diltiazem and erythromycin may increase ibrutinib systemic exposure (AUC) by 6- to 9-fold under fasting condition. The safety and efficacy of these exposures are unknown. The highest ibrutinib dose evaluated in clinical trials was 12.5 mg/kg (actual doses of 840 to 1400 mg) given for 28 days, which yielded single dose AUC values that were approximately 50% greater than steady-state exposures seen at the highest indicated dose of 560 mg.
ADJUST DOSING INTERVAL: Food increases the oral bioavailability of ibrutinib. The mechanism of interaction is unknown. According to the product labeling, administration with food increases ibrutinib exposure approximately 2-fold compared to administration after overnight fasting.
MANAGEMENT: Patients treated with ibrutinib should avoid consumption of Seville oranges, grapefruit, grapefruit juice, and any supplement containing grapefruit extract. Ibrutinib should be taken once daily at approximately the same time each day.
References
- Cerner Multum, Inc. "UK Summary of Product Characteristics."
- (2013) "Product Information. Imbruvica (ibrutinib)." Pharmacyclics Inc
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
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