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Drug Interactions between bexarotene and gefitinib

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

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Interactions between your drugs

Moderate

bexarotene gefitinib

Applies to: bexarotene and gefitinib

MONITOR: Coadministration with inducers of CYP450 3A4 may decrease the plasma concentrations of gefitinib, which is primarily metabolized by the isoenzyme. When a single 500 mg dose of gefitinib was administered following pretreatment with the potent CYP450 3A4 inducer rifampin (600 mg once daily for 16 days) in healthy male volunteers, mean gefitinib systemic exposure (AUC) decreased by 83% compared to administration of gefitinib alone. The interaction has not been studied with other, less potent inducers.

MANAGEMENT: The potential for diminished pharmacologic effects of gefitinib should be considered during coadministration with CYP450 3A4 inducers. Pharmacologic response to gefitinib should be monitored more closely whenever a CYP450 3A4 inducer is added to or withdrawn from therapy, and the gefitinib dosage adjusted as necessary.

References (5)
  1. Li J, Zhao M, He P, Hidalgo M, Baker SD (2007) "Differential metabolism of gefitinib and erlotinib by human cytochrome p450 enzymes." Clin Cancer Res, 13, p. 3731-7
  2. (2023) "Product Information. Iressa (gefitinib)." Astra-Zeneca Pharmaceuticals
  3. (2022) "Product Information. Apo-Gefitinib (gefitinib)." Apotex Inc
  4. (2023) "Product Information. Iressa (gefitinib)." AstraZeneca UK Ltd
  5. (2021) "Product Information. Iressa (gefitinib)." AstraZeneca Pty Ltd

Drug and food interactions

Moderate

bexarotene food

Applies to: bexarotene

ADJUST DOSING INTERVAL: Food may enhance the oral bioavailability of bexarotene. In one clinical study, bexarotene peak plasma concentration (Cmax) and systemic exposure (AUC) resulting from a 75 to 300 mg dose were 35% and 48% higher, respectively, when administered after a fat-containing meal relative to a glucose solution. In all clinical trials, patients were instructed to take bexarotene with or immediately following a meal.

Coadministration with inhibitors of CYP450 3A4 such as grapefruit juice may theoretically increase the plasma concentrations of bexarotene. In vitro studies suggest that bexarotene is metabolized by CYP450 3A4. However, concomitant administration with multiple doses of ketoconazole, a potent CYP450 3A4 inhibitor, did not alter bexarotene plasma concentrations, which would imply that bexarotene elimination is not substantially dependent on CYP450 3A4 metabolism in vivo.

MANAGEMENT: Because safety and efficacy data are based upon administration with food, bexarotene should be administered once daily with a meal. Patients may want to avoid consuming large amounts of grapefruit or grapefruit juice.

References (2)
  1. (2001) "Product Information. Targretin (bexarotene)." Ligand Pharmaceuticals
  2. Cerner Multum, Inc. "UK Summary of Product Characteristics."

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.

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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

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