Bexarotene with Paclitaxel Interaction Details
Brand Names Associated with Bexarotene
- Bexarotene
- Targretin® Capsules
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Mar 04, 2024
Interaction Effect
Decreased paclitaxel plasma concentrations and increased bexarotene plasma concentrations (concomitant paclitaxel plus carboplatin)
Interaction Summary
Use caution when bexarotene is used concomitantly with paclitaxel (with or without carboplatin). Drug interaction studies demonstrated that concomitant administration of paclitaxel and bexarotene decreased the exposure (AUC) of paclitaxel by 19%, most likely due to induction of CYP3A4-mediated paclitaxel metabolism by bexarotene. When bexarotene was coadministered with paclitaxel plus carboplatin, the AUC and Cmax of bexarotene were increased by 2-fold, most likely due to inhibition of CYP3A4-mediated bexarotene metabolism by paclitaxel. No effect on carboplatin AUC was noted when bexarotene was given with carboplatin alone[1]. Monitor for increased bexarotene side effects when paclitaxel plus carboplatin is coadministered. Monitor for decreased efficacy of paclitaxel when used alone with bexarotene.
Severity
Major
Onset
Unspecified
Evidence
Probable
How To Manage Interaction
Use caution when bexarotene is used concomitantly with paclitaxel (with or without carboplatin). Concomitant use of bexarotene and paclitaxel may result in decreased paclitaxel concentrations. When bexarotene is coadministered with paclitaxel plus carboplatin, increased bexarotene plasma concentrations may occur[1]. Monitor for increased bexarotene side effects when paclitaxel plus carboplatin is coadministered. Monitor for decreased efficacy of paclitaxel when used alone with bexarotene.
Mechanism Of Interaction
Induction of CYP3A4-mediated paclitaxel metabolism by bexarotene; unknown mechanism for increased bexarotene plasma concentrations
Literature Reports
A) In clinical studies, concomitant administration of paclitaxel 200 mg/m(2) IV over 3 hours and bexarotene 400 mg/m(2) orally once daily decreased the exposure (AUC) of paclitaxel by 19% [1].
B) In clinical studies, concomitant administration of paclitaxel 200 mg/m(2) IV over 3 hours plus carboplatin (dose to achieve an AUC of 6 mg x min/mL) and bexarotene 400 mg/m(2) orally once daily increased the AUC(0 to 24 hours) and Cmax of bexarotene by 2-fold compared with bexarotene given alone. Of note, concomitant use of bexarotene and carboplatin alone had no effect on carboplatin AUC [1].
References
1 ) Product Information: Targretin(R) oral capsules, bexarotene oral capsules. Eisai Inc. (per FDA), Woodcliff Lake, NJ, 2011.
Bexarotene Overview
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Bexarotene is used to treat cutaneous T-cell lymphoma (CTCL, a type of skin cancer) in people whose disease could not be treated successfully with at least one other medication. Bexarotene is in a class of medications called retinoids. It works by stopping the growth of cancer cells.
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Definitions
Severity Categories
Contraindicated
These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.
Major
This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.
Moderate
This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.
Minor
While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.
Onset
Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.
Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.
Evidence
Level of documentation of the interaction.
Established: The interaction is documented and substantiated in peer-reviewed medical literature.
Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.
How To Manage The Interaction
Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.
It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.
Mechanism Of Interaction
The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.
Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.
Where Does Our Information Come From?
Information for our drug interactions is compiled from several drug compendia, including:
The prescribing information for each drug, as published on DailyMED, is also used.
Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.
The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.