Pralsetinib with Bosentan Interaction Details
Brand Names Associated with Pralsetinib
- Gavreto®
- Pralsetinib
Brand Names Associated with Bosentan
- Bosentan
- Tracleer®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Dec 26, 2023
Interaction Effect
Reduced pralsetinib exposure and reduced efficacy of pralsetinib
Interaction Summary
Coadministration of pralsetinib (a CYP3A substrate) with a moderate CYP3A inducer may result in decreased pralsetinib exposure, which may decrease the efficacy of pralsetinib. Avoid concomitant use. If coadministration cannot be avoided, increase the starting dose of pralsetinib (i.e., from 400 mg once daily to 600 mg once daily; 300 mg once daily to 500 mg once daily and 200 mg once daily to 300 mg once daily) starting on Day 7 of coadministration with the moderate CYP3A inducer. After the moderate CYP3A inducer has been discontinued for at least 14 days, resume the dose of pralsetinib that was taken prior to initiating the moderate CYP3A inducer.
Severity
Major
Onset
Unspecified
Evidence
Theoretical
How To Manage Interaction
Coadministration of pralsetinib (a CYP3A substrate) with a moderate CYP3A inducer may result in decreased pralsetinib exposure, which may decrease the efficacy of pralsetinib. Avoid concomitant use. If coadministration cannot be avoided, increase the starting dose of pralsetinib (i.e., from 400 mg once daily to 600 mg once daily; 300 mg once daily to 500 mg once daily and 200 mg once daily to 300 mg once daily) starting on Day 7 of coadministration with the moderate CYP3A inducer. After the moderate CYP3A inducer has been discontinued for at least 14 days, resume the dose of pralsetinib that was taken prior to initiating the moderate CYP3A inducer.
Mechanism Of Interaction
Induction of CYP3A-mediated metabolism of pralsetinib
Literature Reports
A) Coadministration of multiple doses of efavirenz 600 mg once daily (moderate CYP3A inducer) is predicted to decrease the pralsetinib Cmax by 18% and AUC by 45% .
Pralsetinib Overview
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Pralsetinib is used to treat a certain type of non small-cell lung cancer (NSCLC) in adults that has spread to other parts of the body. It is also used to treat a certain type of thyroid cancer in adults and children 12 years of age and older that is getting worse or that has spread to other parts of the body. Pralsetinib is used to treat a certain type of thyroid cancer in adults and children 12 years of age and older that is getting worse or that has spread to other parts of the body and cannot be treated with radioactive iodine. Pralsetinib is in a class of medications called kinase inhibitors. It works by blocking the action of a certain naturally occurring substance that may be needed to help cancer cells multiply.
Bosentan Overview
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Bosentan is used to treat pulmonary arterial hypertension (PAH, high blood pressure in the vessels that carry blood to the lungs) in adults and children 3 years of age and older. Bosentan may improve the ability to exercise and slow the worsening of symptoms in patients with PAH. Bosentan is in a class of medications called endothelin receptor antagonists. It works by stopping the action of endothelin, a natural substance that causes blood vessels to narrow and prevents normal blood flow in people who have PAH.
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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.