Fluconazole with Tazemetostat Interaction Details
Brand Names Associated with Fluconazole
- Diflucan®
- Fluconazole
Brand Names Associated with Tazemetostat
- Tazemetostat
- Tazverik®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Dec 19, 2023
Interaction Effect
Increased tazemetostat expsoure and risk of toxicity
Interaction Summary
Concomitant use of tazemetostat with a moderate CYP3A inhibitor (fluconazole) significantly increased tazemetostat exposure in a pharmacokinetic study. Coadministration may increase the frequency or severity of tazemetostat-associated adverse events and should be avoided. If coadministration is required, reduce tazemetostat based upon current dosage: from 800 mg twice daily to 400 mg twice daily; from 600 mg twice daily to 400 mg for the first dose and 200 mg for the second dose daily; and from 400 mg twice daily to 200 mg twice daily. After discontinuation of the moderate CYP3A inhibitor for 3 elimination half-lives, resume the tazemetostat dosage that was taken prior to concurrent use.
Severity
Major
Onset
Unspecified
Evidence
Theoretical
How To Manage Interaction
Concomitant use of tazemetostat with a moderate CYP3A inhibitor may significantly increase tazemetostat plasma concentrations, which may increase the risk of tazemetostat-associated adverse events. Concomitant use should be avoided. If coadministration is required, reduce tazemetostat based upon current dosage: from 800 mg twice daily to 400 mg twice daily; from 600 mg twice daily to 400 mg for the first dose and 200 mg for the second dose daily; and from 400 mg twice daily to 200 mg twice daily. After discontinuation of the moderate CYP3A inhibitor for 3 elimination half-lives, resume the tazemetostat dosage that was taken prior to initiating the inhibitor.
Mechanism Of Interaction
Inhibition of CYP3A-mediated tazemetostat metabolism
Literature Reports
A) Concomitant use of tazemetostat 400 mg twice daily with fluconazole (a moderate CYP3A inhibitor) increased tazemetostat steady-state AUC(0 to 8) by 3.1-fold and Cmax by 2.3-fold .
Fluconazole Overview
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Fluconazole is used to treat fungal infections, including yeast infections of the vagina, mouth, throat, esophagus (tube leading from the mouth to the stomach), abdomen (area between the chest and waist), lungs, blood, and other organs. Fluconazole is also used to treat meningitis (infection of the membranes covering the brain and spine) caused by fungus. Fluconazole is also used to prevent yeast infections in patients who are likely to become infected because they are being treated with chemotherapy or radiation therapy before a bone marrow transplant (replacement of unhealthy spongy tissue inside the bones with healthy tissue). Fluconazole is in a class of antifungals called triazoles. It works by slowing the growth of fungi that cause infection.
Tazemetostat Overview
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Tazemetostat is used to treat epithelioid sarcoma (a rare, slow-growing soft tissue cancer) in adults and children 16 years of age and older that has spread to nearby tissues or to other parts of the body and cannot be treated successfully with surgery. It is also used to treat certain types of follicular lymphoma (FL; a type of cancer that begins in the white blood cells) in adults whose cancer that has returned or did not respond to at least two other medications. Tazemetostat is also used to treat follicular lymphoma in adults that has returned or did not respond to treatment when no other treatment options are available. Tazemetostat is in a class of medications called EZH2 inhibitors. It helps to stop the spread 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.