Neratinib with Idelalisib Interaction Details


Brand Names Associated with Neratinib

  • Neratinib
  • Nerlynx®

Brand Names Associated with Idelalisib

  • Idelalisib
  • Zydelig®

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Last updated Dec 29, 2023


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Interaction Effect

Increased neratinib exposure and risk of toxicity


Interaction Summary

Concomitant use of neratinib (a CYP3A4 substrate) with strong CYP3A4 inhibitors increases neratinib exposure and may increase the risk of toxicity and therefore should be avoided. In a pharmacokinetic study, a single dose of neratinib given concomitantly with daily ketoconazole (a strong CYP3A4 inhibitor) increased the neratinib Cmax by 221% and the AUC by 381% in healthy subjects.


Severity

Major


Onset

Unspecified


Evidence

Theoretical


How To Manage Interaction

Avoid the concomitant use of neratinib (a CYP3A4 substrate) with strong CYP3A4 inhibitors due to increases in neratinib exposure and an increased risk of toxicity.


Mechanism Of Interaction

Inhibition of CYP3A4-mediated neratinib metabolism


Literature Reports

A) Coadministration of a single oral dose of neratinib 240 mg with ketoconazole 400 mg orally once daily for 5 days (a strong CYP3A4 inhibitor) increased the neratinib Cmax by 221% and the AUC by 381% in a drug interaction study in healthy subjects (N=24) .

Neratinib Overview

  • Neratinib is used to treat a certain type of hormone receptor-positive breast cancer (breast cancer that depends on hormones such as estrogen to grow) in adults after treatment with trastuzumab (Herceptin) and other medications. Neratinib is used along with capecitabine (Xeloda) to treat a certain type of advanced hormone receptor-positive breast cancer or breast cancer that has spread to other parts of the body after treatment with at least two other medications. Neratinib is in a class of medications called kinase inhibitors. It works by blocking the action of an abnormal protein that signals cancer cells to multiply. This helps slow or stop the spread of cancer cells.

See More information Regarding Neratinib

Idelalisib Overview

  • Idelalisib is used along with another medication rituximab (Rituxan) to treat chronic lymphocytic leukemia (CLL; a type of cancer that begins in the white blood cells) in people whose cancer came back after receiving other cancer treatments. It is also used to treat certain types of follicular lymphoma (FL; a type of cancer that begins in the white blood cells) and small lymphocytic lymphoma (SLL:a type of cancer that begins in the white blood cells) in people whose cancer came back after being treated with at least 2 other cancer treatments. Idelalisib 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 the spread of cancer cells.

See More information Regarding Idelalisib

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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.