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Drug Interactions between bexarotene and fostemsavir

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

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Interactions between your drugs

Minor

bexarotene fostemsavir

Applies to: bexarotene and fostemsavir

Coadministration of fostemsavir with moderate or weak CYP450 3A4 inducers may decrease the plasma concentrations of temsavir, the active moiety of fostemsavir. According to the prescribing information, temsavir is a substrate of CYP450 3A4, esterases, P-glycoprotein (P-gp), and breast cancer resistance protein (BCRP). When fostemsavir (600 mg twice daily) was coadministered with the moderate CYP450 3A4 inducer etravirine (200 mg twice daily) in 14 study subjects, mean temsavir peak plasma concentration (Cmax), systemic exposure (AUC) and trough plasma concentration (Ctau) decreased by 48%, 50% and 52%, respectively, compared to fostemsavir administered alone. When the same dosage of fostemsavir was given to 22 study subjects with another moderate CYP450 3A4 inducer, rifabutin (300 mg once daily), mean temsavir Cmax, AUC and Ctau decreased by 27%, 30% and 41%, respectively. These changes are not considered clinically relevant, and no dosage adjustment of fostemsavir is recommended when coadministered with moderate or weak CYP450 3A4 inducers.

References (3)
  1. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  2. Cerner Multum, Inc. "Australian Product Information."
  3. (2020) "Product Information. Rukobia (fostemsavir)." ViiV Healthcare

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

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

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