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Drug Interactions between pexidartinib and temsirolimus

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

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Interactions between your drugs

Moderate

temsirolimus pexidartinib

Applies to: temsirolimus and pexidartinib

GENERALLY AVOID: Coadministration of temsirolimus with inducers of CYP450 3A4 may decrease the plasma concentrations of sirolimus, a major active metabolite of temsirolimus and known substrate of CYP450 3A4. According to the product labeling, administration of temsirolimus in combination with the potent CYP450 3A4 inducer rifampin, resulted in a 65% and 56% decrease in sirolimus peak plasma concentration (Cmax) and systemic exposure (AUC), respectively, compared to administration of temsirolimus alone. No significant effect on the pharmacokinetics of temsirolimus was reported. The extent to which other inducers of CYP450 3A4 interact with temsirolimus is unknown.

MANAGEMENT: In the setting of mantle cell lymphoma, concomitant use of temsirolimus with inducers of CYP450 3A4 should generally be avoided. When used for the treatment of renal cell carcinoma, some authorities advise a dose increase from the recommended 25 mg IV once weekly to 50 mg IV once weekly depending on patient tolerability. Based on pharmacokinetic studies, this dosage is predicted to adjust the sirolimus AUC to the range observed without inducers; however, clinical data are lacking. The dosage should be reduced to the normally recommended dose following discontinuation of the potent CYP450 3A4 inducer. Other authorities also advise that temsirolimus should not be used in combination with CYP450 3A4 inducers for longer than 5 to 7 days in these patients.

References (3)
  1. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  2. (2007) "Product Information. Torisel (temsirolimus)." Wyeth-Ayerst Laboratories
  3. Cerner Multum, Inc. "Australian Product Information."

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

temsirolimus food

Applies to: temsirolimus

GENERALLY AVOID: Coadministration of temsirolimus with grapefruit juice may increase the plasma concentrations of sirolimus, a major active metabolite of temsirolimus and known substrate of CYP450 3A4. The proposed mechanism is inhibition of CYP450 3A4-mediated metabolism by certain compounds present in grapefruits.

MANAGEMENT: Patients treated with temsirolimus should preferably avoid the consumption of grapefruit or grapefruit juice.

References (1)
  1. (2007) "Product Information. Torisel (temsirolimus)." Wyeth-Ayerst Laboratories

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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