Abemaciclib and Ketoconazole: Drug Interaction Guide

Quick answer: This is a major interaction — avoid combining Abemaciclib and Ketoconazole unless specifically directed by your doctor.

Interaction severity: Major — avoid combination

How Abemaciclib interacts with Ketoconazole

Ketoconazole strongly inhibits CYP3A4-mediated metabolism of abemaciclib, increasing exposure 16-fold and risk of severe neutropenia, diarrhea, and hepatotoxicity.

What you should do

Avoid concomitant strong CYP3A4 inhibitors; if unavoidable, reduce abemaciclib dose to 50 mg twice daily.

Key facts

Severity

Major — avoid combination

Mechanism

Ketoconazole strongly inhibits CYP3A4-mediated metabolism of abemaciclib, increasing exposure 16-fold and risk of severe...

Action

Avoid concomitant strong CYP3A4 inhibitors; if unavoidable, reduce abemaciclib dose to 50 mg twice daily.

Important medical disclaimer: This page provides educational information about drug interactions for general reference. It is not a substitute for professional medical advice, diagnosis, or treatment. Always discuss your specific medications with a qualified healthcare provider before starting, stopping, or changing any treatment. About our editorial team.

Frequently asked questions

Can I take Abemaciclib and Ketoconazole together?

No — this combination should generally be avoided. Avoid concomitant strong CYP3A4 inhibitors; if unavoidable, reduce abemaciclib dose to 50 mg twice daily.

What is the severity of this interaction?

The interaction between Abemaciclib and Ketoconazole is classified as Major — avoid combination. Ketoconazole strongly inhibits CYP3A4-mediated metabolism of abemaciclib, increasing exposure 16-fold and risk of severe neutropenia, diarrhea, and hepatotoxicity.

What should I do if I'm prescribed both?

Avoid concomitant strong CYP3A4 inhibitors; if unavoidable, reduce abemaciclib dose to 50 mg twice daily. Always consult your prescribing clinician — do not stop or change medications without medical guidance.

Last reviewed: by iMedic Medical Editorial Team. Our editorial process.