Crizotinib with Abemaciclib Interaction Details

Brand Names Associated with Crizotinib

Brand Names Associated with Abemaciclib

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Feb 25, 2024

Interaction Effect

Increased abemaciclib plasma concentration

Interaction Summary

Concomitant use of abemaciclib (a CYP3A4 substrate) and a moderate CYP3A4 inhibitor may result in increased plasma levels of abemaciclib and its active metabolite, and may lead to increased toxicity. If coadministered, monitor for adverse reactions and consider reducing the dose of abemaciclib in 50-mg increments (for patients receiving 150 mg twice daily: first reduction to 100 mg twice daily; second reduction to 50 mg twice daily; discontinue use if 50 mg twice daily is not tolerated; for patients receiving 200 mg twice daily: first reduction to 150 mg twice daily; second reduction to 100 mg twice daily; third reduction to 50 mg twice daily; discontinue use if 50 mg twice daily is not tolerated)[1].

Severity

Moderate

Onset

Unspecified

Evidence

Theoretical

How To Manage Interaction

Concomitant use of abemaciclib (a CYP3A4 substrate) and a moderate CYP3A4 inhibitor may result in increased plasma levels of abemaciclib and its active metabolite, and may lead to increased toxicity. If coadministered, monitor for adverse reactions and consider reducing the dose of abemaciclib in 50-mg increments (for patients receiving 150 mg twice daily: first reduction to 100 mg twice daily; second reduction to 50 mg twice daily; discontinue use if 50 mg twice daily is not tolerated; for patients receiving 200 mg twice daily: first reduction to 150 mg twice daily; second reduction to 100 mg twice daily; third reduction to 50 mg twice daily; discontinue use if 50 mg twice daily is not tolerated)[1].

Mechanism Of Interaction

Inhibition of CYP3A4-mediated abemaciclib metabolism

Literature Reports

A) In drug interaction studies, concomitant use of abemaciclib with verapamil and diltiazem (moderate CYP3A inhibitors) is predicted to increase the AUC of abemaciclib plus its active metabolites (M2, M18 and M20) by approximately 1.6-fold and 2.4-fold, respectively [1].

References

1 ) Product Information: VERZENIO(TM) oral tablets, abemaciclib oral tablets. Lilly USA LLC (per FDA), Indianapolis, IN, 2018.

Crizotinib Overview

• Crizotinib is used to treat certain types of non-small cell lung cancer (NSCLC) that has spread to nearby tissues or to other parts of the body. It is also used to treat a certain type of anaplastic large cell lymphoma (ALCL) that has returned or is unresponsive to other treatment(s) in certain adults and children 1 year of age and older. Crizotinib is also used to treat a certain type of inflammatory myofibroblastic tumor (IMT; type of cancer that occurs in mucosal tissues usually in the abdominal area, involving the lungs, bladder, stomach, uterus, liver, or intestines) that cannot be treated with surgery or that has not improved or has come back after previous treatment(s) in adults and children 1 year of age and older. Crizotinib 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.

Abemaciclib Overview

• Abemaciclib is used in combination with an aromatase inhibitor such as anastrozole (Arimidex), exemestane (Aromasin), or letrozole (Femara) to treat a certain type of hormone receptor-positive, early breast cancer. Abemaciclib is also used along with fulvestrant (Faslodex) to treat a certain type of hormone receptor-positive, advanced breast cancer (breast cancer that depends on hormones such as estrogen to grow) or breast cancer that has spread to other parts of the body after treatment with an antiestrogen medication such as tamoxifen. Abemaciclib is also used along with anastrozole (Arimidex), exemestane (Aromasin), or letrozole (Femara) as a first treatment of hormone receptor-positive, advanced breast cancer or breast cancer that has spread to other parts of the body. Abemaciclib is also used alone to treat a certain type of hormone receptor-positive, advanced breast cancer or breast cancer that has spread to other parts of the body in people who have already been treated with an antiestrogen medication and chemotherapy. Abemaciclib 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.

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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:

• Gold Standard Drug Database
• Micromedex
• Lexicomp
• DrugBank

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.