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Brukinsa and Alcohol/Food Interactions

There are 2 alcohol/food/lifestyle interactions with Brukinsa (zanubrutinib).

Major

Zanubrutinib Food

Major Food Interaction

GENERALLY AVOID: Grapefruit and/or grapefruit juice may increase the plasma concentrations of zanubrutinib. 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 grapefruit juice, but has been reported for other CYP450 3A4 inhibitors. When zanubrutinib was administered with the potent CYP450 3A4 inhibitor itraconazole (200 mg once daily) in clinical study subjects, zanubrutinib peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 157% and 278%, respectively. Data derived from pharmacokinetic modeling have also been reported for several additional CYP450 3A4 inhibitors. For example, the potent CYP450 3A4 inhibitor clarithromycin (250 mg twice daily) is predicted to increase zanubrutinib Cmax and AUC by 175% and 183%, respectively. The moderate CYP450 3A4 inhibitor diltiazem (60 mg three times daily) is predicted to increase zanubrutinib Cmax and AUC by 151% and 157%, respectively. Another moderate CYP450 3A4 inhibitor, erythromycin (500 mg four times daily), is predicted to increase zanubrutinib Cmax and AUC by 284% and 317%, respectively. Likewise, fluconazole 200 mg once daily is predicted to increase zanubrutinib Cmax and AUC by 179% and 177%, respectively; while fluconazole 400 mg once daily is predicted to increase zanubrutinib Cmax and AUC by 270% and 284%, respectively. In general, the effects of grapefruit products are concentration-, dose- and preparation-dependent, and can vary widely among brands. Certain preparations of grapefruit (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 zanubrutinib exposure may potentiate the risk of toxicities such as hemorrhage, infection, cytopenias, malignancies, and serious cardiac arrhythmias (primarily atrial fibrillation and atrial flutter).

Food does not affect the oral bioavailability of zanubrutinib. No clinically significant differences in zanubrutinib Cmax or AUC were observed following administration of a high-fat meal (approximately 1000 calories; 50% from fat) in healthy subjects.

MANAGEMENT: Zanubrutinib may be administered with or without food. Patients should avoid consumption of grapefruit, grapefruit juice, Seville oranges, and Seville orange juice during treatment with zanubrutinib.

References

  1. (2023) "Product Information. Brukinsa (zanubrutinib)." BeiGene USA, Inc, SUPPL-7
  2. (2022) "Product Information. Brukinsa (zanubrutinib)." Innomar Strategies Inc.
  3. (2022) "Product Information. Brukinsa (zanubrutinib)." Beigene Aus Pty Ltd

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Moderate

Zanubrutinib High Blood Pressure (Hypertension)

Moderate Potential Hazard, Moderate plausibility

zanubrutinib - arrhythmias

Serious cardiac arrhythmias have been reported with zanubrutinib. Atrial fibrillation and atrial flutter have occurred in patients treated with zanubrutinib monotherapy. Care should be exercised when using this agent in patients with cardiac risk factors, hypertension, and acute infections as they may be at increased risk of cardiac arrhythmias. It is recommended to monitor for signs/symptoms of cardiac arrhythmias, manage appropriately, and consider the risks and benefits of continued treatment with zanubrutinib.

References

  1. (2023) "Product Information. Brukinsa (zanubrutinib)." BeiGene USA, Inc, SUPPL-10

Brukinsa drug interactions

There are 459 drug interactions with Brukinsa (zanubrutinib).

Brukinsa disease interactions

There are 6 disease interactions with Brukinsa (zanubrutinib) which include:


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Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor 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.
Unknown No interaction information available.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.