Belzutifan with Fentanyl Interaction Details
Brand Names Associated with Belzutifan
- Belzutifan
- Welireg®
Brand Names Associated with Fentanyl
- Abstral®
- Actiq®
- Fentanyl
- Fentora®
- Onsolis®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Dec 31, 2023
Interaction Effect
Reduced exposure to CYP3A substrate
Interaction Summary
Coadministration of belzutifan with CYP3A4 substrates decreases concentrations of the CYP3A substrates, which may reduce the efficacy of these substrates. The magnitude of this effect may be more pronounced in patients who are dual UGT2B17 and CYP2C19 poor metabolizers. Coadministration of belzutifan with midazolam (a sensitive CYP3A4 substrate) decreased the midazolam AUC by 40% and the Cmax by 34%. Midazolam AUC is predicted to decrease up to 70% in patients with higher belzutifan concentrations (eg, dual poor metabolizers). Avoid coadministration of belzutifan with sensitive CYP3A4 substrates, for which minimal decrease in concentration may lead to therapeutic failures of the substrate. If coadministration cannot be avoided, increase the sensitive CYP3A4 substrate dosage in accordance with its prescribing information.
Severity
Major
Onset
Unspecified
Evidence
Theoretical
How To Manage Interaction
Coadministration of belzutifan with CYP3A4 substrates decreases concentrations of the CYP3A substrates, which may reduce the efficacy of these substrates. The magnitude of this effect may be more pronounced in patients who are dual UGT2B17 and CYP2C19 poor metabolizers. Avoid coadministration of belzutifan with sensitive CYP3A4 substrates, for which minimal decrease in concentration may lead to therapeutic failures of the substrate. If coadministration cannot be avoided, increase the sensitive CYP3A4 substrate dosage in accordance with its prescribing information.
Mechanism Of Interaction
Induction of CYP3A-mediated metabolism by belzutifan
Literature Reports
A) Coadministration of belzutifan 120 mg once daily with midazolam (a sensitive CYP3A4 substrate) decreased the midazolam AUC by 40% and the Cmax by 34%. Midazolam AUC is predicted to decrease up to 70% in patients with higher belzutifan concentrations (eg, dual poor metabolizers) .
Belzutifan Overview
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Belzutifan is used in adults with von Hippel-Lindau disease (VHL; a rare disease that causes tumors and cysts) to treat renal cell carcinoma (RCC; kidney cancer), central nervous system (CNS) hemangioblastomas (tumors in the brain and spinal cord), and a certain type of pancreatic cancer that does not require surgery right away. Belzutifan is in a class of medications called hypoxia-inducible factor inhibitors. It works by blocking the activity of a certain protein in people with VHL.
Fentanyl Overview
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Fentanyl is used to treat breakthrough pain (sudden episodes of pain that occur despite round the clock treatment with pain medication) in cancer patients at least 18 years of age (or at least 16 years of age if using Actiq brand lozenges) who are taking regularly scheduled doses of another narcotic (opiate) pain medication, and who are tolerant (used to the effects of the medication) to narcotic pain medications. Fentanyl is in a class of medications called narcotic (opiate) analgesics. It works by changing the way the brain and nervous system respond to pain.
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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.