Lapatinib with Pralsetinib Interaction Details
Brand Names Associated with Lapatinib
- Lapatinib
- Tykerb®
Brand Names Associated with Pralsetinib
- Gavreto®
- Pralsetinib
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Dec 26, 2023
Interaction Effect
Increased pralsetinib exposure and an increased risk of pralsetinib-related adverse events
Interaction Summary
Coadministration of pralsetinib (a P-gp substrate) and P-gp inhibitors may increase pralsetinib exposure, which may increase the incidence and severity of adverse reactions. Coadministration of cycloSPORINE with pralsetinib in healthy subjects increased pralsetinib AUC(0 to inf) by 81% and Cmax by 48%, relative to pralsetinib administered alone. Avoid concomitant use of pralsetinib with P-gp inhibitors. If coadministration cannot be avoided, reduce the pralsetinib dose in patients taking 400 mg, 300 mg and 200 mg orally once daily to 300 mg, 200 mg and 100 mg orally once daily respectively. After the inhibitor has been discontinued for 3 to 5 elimination half-lives of the inhibitor, resume pralsetinib at the dose taken prior to initiating the inhibitor.
Severity
Major
Onset
Unspecified
Evidence
Probable
How To Manage Interaction
Coadministration of pralsetinib (a P-gp substrate) and P-gp inhibitors may increase pralsetinib exposure, which may increase the incidence and severity of adverse reactions. Avoid concomitant use of pralsetinib with P-gp inhibitors. If coadministration cannot be avoided, reduce the pralsetinib dose in patients taking 400 mg, 300 mg and 200 mg orally once daily to 300 mg, 200 mg and 100 mg orally once daily respectively. After the inhibitor has been discontinued for 3 to 5 elimination half-lives of the inhibitor, resume pralsetinib at the dose taken prior to initiating the inhibitor.
Mechanism Of Interaction
Inhibition of P-gp-mediated efflux transport of pralsetinib
Literature Reports
A) Coadministration of cycloSPORINE (single 600 mg dose) with a single 200 mg dose of pralsetinib in healthy subjects increased pralsetinib AUC(0 to inf) by 81% and Cmax by 48%, relative to a 200 mg dose of pralsetinib administered alone .
B) In the clinical studies, coadministration of itraconazole (a combined P-gp and strong CYP3A inhibitor) 200 mg twice daily on Day 1 followed by 200 mg once daily with pralsetinib increased pralsetinib Cmax by 84% and AUC by 251% .
C) In a model-informed approach, coadministration of verapamil (a combined P-gp and moderate CYP3A inhibitor) 80 mg thrice daily with pralsetinib is predicted to increase pralsetinib Cmax by 60% and AUC by 108% .
Lapatinib Overview
-
Lapatinib is used with capecitabine (Xeloda) to treat a certain type of advanced breast cancer in people who have already been treated with other chemotherapy medications. Lapatinib is also used with letrozole (Femara) to treat a certain type of breast cancer in postmenopausal women (women who have experienced a change of life; end of menstrual periods) that has spread to other parts of the body. Lapatinib is in a class of medications called kinase inhibitors. It works by blocking the action of the abnormal protein that signals cancer cells to multiply. This helps stop or slow the spread of cancer cells.
Pralsetinib Overview
-
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.
Return To Our Drug Interaction Homepage
Feedback, Question Or Comment About This Information?
Ask Dr. Brian Staiger, PharmD, our medical editor, directly! He's always more than happy to assist.
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.