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Drug Interactions between Brilinta and pexidartinib

This report displays the potential drug interactions for the following 2 drugs:

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Interactions between your drugs

Moderate

ticagrelor pexidartinib

Applies to: Brilinta (ticagrelor) and pexidartinib

GENERALLY AVOID: Coadministration with inducers of CYP450 3A4 may decrease the plasma concentrations of ticagrelor, which is primarily metabolized by the isoenzyme. In 14 healthy volunteers, administration of a single 180 mg oral dose of ticagrelor on day 12 of treatment with the potent CYP450 3A4 inducer rifampin (600 mg once daily for 14 days) decreased mean ticagrelor peak plasma concentration (Cmax), systemic exposure (AUC) and plasma half-life by 73%, 86% and 67%, respectively, compared to administration of ticagrelor alone. Mean Cmax of the major active metabolite was unchanged in the presence of rifampin, but mean AUC decreased by 46% and plasma half-life by 50%. Inhibition of platelet aggregation (IPA) was also assessed in the study. Mean IPA at 12 hours was 87% with ticagrelor alone versus 63% in combination with rifampin; corresponding values at 24 hours were 70% and 15%, respectively. It is not known to what extent ticagrelor may interact with weak and moderate CYP450 3A4 inducers.

MANAGEMENT: Concomitant use of ticagrelor with CYP450 3A4 inducers should generally be avoided. Otherwise, caution is advised, and patients should be closely monitored for diminished clinical response to ticagrelor therapy. Alternative treatment may be required if an interaction is suspected.

References

  1. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  2. Canadian Pharmacists Association (2006) e-CPS. http://www.pharmacists.ca/function/Subscriptions/ecps.cfm?link=eCPS_quikLink
  3. (2011) "Product Information. Brilinta (ticagrelor)." Astra-Zeneca Pharmaceuticals
  4. Teng R, Mitchell P, Butler K (2013) "Effect of rifampicin on the pharmacokinetics and pharmacodynamics of ticagrelor in healthy subjects." Eur J Clin Pharmacol, 69, p. 877-83
  5. Weeks P, Sieg A, Vahdat K, Raissi F, Nathan S (2014) "Improved ticagrelor antiplatelet effect on discontinuation of phenytoin." Ann Pharmacother, 48, p. 644-7
View all 5 references

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Drug and food interactions

Major

pexidartinib food

Applies to: pexidartinib

ADJUST DOSING INTERVAL: The presence of food may increase the absorption and toxicity of pexidartinib. Administration of pexidartinib with a high-fat meal increased peak plasma concentration (Cmax) and systemic exposure (AUC) by 100% and prolonged the time to reach peak plasma concentration (Tmax) by 2.5 hours.

GENERALLY AVOID: Grapefruit or grapefruit juice may increase the plasma concentration and risk of adverse effects of pexidartinib, including potentially fatal hepatotoxicity. The mechanism is inhibition of CYP450 3A4-mediated metabolism of pexidartinib by certain compounds present in grapefruits. Concomitant administration of itraconazole, a strong CYP450 3A4 inhibitor, increased pexidartinib peak plasma concentration (Cmax) and systemic exposure (AUC) by 48% and 70%, respectively.

MANAGEMENT: Pexidartinib should be administered on an empty stomach, at least one hour before or two hours after a meal or snack. Consumption of grapefruit or grapefruit juice should generally be avoided during pexidartinib therapy. If concomitant use is unavoidable, the dose of pexidartinib should be reduced according to the manufacturer's recommendations. If concomitant use of grapefruit or grapefruit juice is discontinued, the dose of pexidartinib may be increased (after 3 plasma half-lives of a strong CYP450 3A4 inhibitor) to the dose that was used prior to consumption of grapefruit or grapefruit juice.

References

  1. (2019) "Product Information. Turalio (pexidartinib)." Daiichi Sankyo, Inc.

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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

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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.

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