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Interactions between Ezetimibe and Rilzabrutinib

1 drug interaction and 4 additional warnings found for the following 2 drugs:

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Drug interactions

Moderate drug interactions

Moderate:

ezetimibe rilzabrutinib

Applies to: ezetimibe and rilzabrutinib
Monitor

Coadministration with rilzabrutinib may increase the plasma concentrations and the risk of adverse effects of drugs that are breast cancer resistance protein (BCRP), organic anion-transporting polypeptide (OATP1B1/3), P-glycoprotein (P-gp), and/or bile salt export pump (BSEP) substrates. According to in vitro data, rilzabrutinib may inhibit these transporters at clinically relevant concentrations. However, the clinical significance of these transporter interactions is currently unknown as clinical data are limited.

Management

Caution is recommended when using rilzabrutinib with drugs that are substrates of BCRP, OATP1B1/3, P-gp, or BSEP, particularly those with a narrow therapeutic index, where minimal changes in concentration may increase the risk of adverse reactions. Monitor patients for increased adverse reactions associated with the concomitant substrate and consider dosage adjustments in accordance with the substrate's product labeling.

References (1)
  1. (2025) "Product Information. Wayrilz (rilzabrutinib)." Genzyme Corporation

Food/lifestyle interactions

Major food/lifestyle interactions

Major:

rilzabrutinib Food/Lifestyle

Applies to: rilzabrutinib
Generally avoid

Grapefruit, grapefruit juice, Seville oranges, and starfruit may increase the plasma concentrations of rilzabrutinib, which is primarily metabolized by CYP450 3A4. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in these fruits. Inhibition of hepatic CYP450 3A4 may also contribute. The interaction has not been studied with grapefruit, Seville oranges, or starfruit but has been studied with other CYP450 3A4 inhibitors. Based on clinical studies, concomitant use with the potent CYP450 3A4 inhibitor ritonavir increased rilzabrutinib peak plasma concentration (Cmax) and systemic exposure (AUC) by 5-fold and 8-fold at steady state, respectively. Based on model-informed approaches, coadministration of moderate CYP450 3A4 inhibitors (e.g., fluconazole, erythromycin, verapamil) is predicted to increase rilzabrutinib Cmax and AUC by 3-fold at steady state. 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 rilzabrutinib may increase the risk of adverse effects such as infections, diarrhea, nausea, and headache.

Management

It may be advisable for patients to avoid the consumption of grapefruit, grapefruit juice, Seville oranges, starfruit or products that contain these fruits during treatment with rilzabrutinib.

References (34)
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Disease interactions

3 potential interactions Applies to: 2 conditions, including Liver Disease and Renal Dysfunction.

Liver Disease

Major:

ezetimibe

Ezetimibe has a major potential interaction with Liver Disease.

Ezetimibe is not recommended for use in patients with moderate to severe hepatic impairment (Child-Pugh B or C) due to the unknown effects of increased exposure in this population.

Moderate:

rilzabrutinib

Rilzabrutinib has a moderate potential interaction with Liver Disease.

Rilzabrutinib is not recommended for use in patients with moderate or severe hepatic dysfunction (Child-Pugh B or C). Cmax and AUC increased by approximately 4.5-fold in patients with moderate hepatic dysfunction. Patients with severe hepatic dysfunction were not studied.

Renal Dysfunction

Moderate:

rilzabrutinib

Rilzabrutinib has a moderate potential interaction with Renal Dysfunction.

Rilzabrutinib is not recommended for use in patients with severe renal dysfunction (CrCl less than 46 mL/min). Patients with severe renal dysfunction were not studied.

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ezetimibe

A total of 72 drugs are known to interact with ezetimibe.

rilzabrutinib

A total of 574 drugs are known to interact with rilzabrutinib.

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.

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