Lapatinib with Rifapentine Interaction Details
Brand Names Associated with Lapatinib
- Lapatinib
- Tykerb®
Brand Names Associated with Rifapentine
- Priftin®
- Rifapentine

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Dec 20, 2023
Interaction Effect
Decreased lapatinib exposure or plasma concentrations
Interaction Summary
In healthy participants, concurrent administration of lapatinib with carbamazepine, a CYP3A4-inducer, led to significantly decreased lapatinib AUC (72%). Although studies have not been conducted with other CYP3A4-inducers, it is recommended that concurrent use of strong CYP3A4 inducers, such as rifapentine, with lapatinib be avoided. However, if these agents must be used concurrently, then depending on tolerability, a gradual titration of lapatinib dose from 1250 mg/day up to 4500 mg/day should be considered. This adjustment is recommended based on pharmacokinetic data and would be expected to adjust lapatinib AUC to the therapeutic ranges achieved without CYP3A4 inducers. However, no clinical data is currently available with such adjustments. If rifapentine is discontinued, the increased lapatinib dose should be reduced to the indicated dose.
Severity
Major
Onset
Unspecified
Evidence
Theoretical
How To Manage Interaction
Coadministration of lapatinib with rifapentine, a CYP3A4-inducer, may result in significantly decreased lapatinib AUC and should be avoided. However, if concurrent use is warranted, then consider titrating the dose of lapatinib gradually from 1250 mg/day up to 4500 mg/day, depending on tolerability. Once rifapentine is discontinued, reduce the increased lapatinib dose to the indicated dose.
Mechanism Of Interaction
Induction of CYP3A4-mediated lapatinib metabolism
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.
Rifapentine Overview
-
Rifapentine is used with other medications to treat active tuberculosis (TB; a serious infection that affects the lungs and sometimes other parts of the body) in adults and children 12 years of age and older. Rifapentine is also used with isoniazid (Laniazid) to treat adults and children 2 years of age and older with latent (resting or nongrowing) TB, including those in close contact with people who have active TB, a positive tuberculin skin test, human immunodeficiency virus (HIV), or those with pulmonary fibrosis (scarring of the lungs with an unknown cause). Rifapentine is in a class of medications called antimycobacterials. It works by killing the bacteria that cause infection.
-
Antibiotics such as rifapentine will not work for colds, flu, or other viral infections. Using antibiotics when they are not needed increases your risk of getting an infection later that resists antibiotic treatment.
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.