Drug interactions
Enzalutamide + Rifampin
Severity: Major
Enzalutamide and Rifampin: major interaction.
Last updated Sources: US FDA label
For healthcare professionals — reference only. This page is a brief summary, not medical advice and not a substitute for official labeling or clinical judgement. Always verify before prescribing or dispensing.
Summary
Rifampin is a strong CYP3A4 and CYP2C8 inducer and can lower enzalutamide and active metabolite exposure. This may reduce the clinical efficacy of prostate cancer therapy.
What this interaction means in plain words
Enzalutamide and Rifampin can interact in a way that may be serious. Using them together is sometimes necessary, but it needs a deliberate decision by the prescriber, a plan for monitoring, and clear advice on the warning signs to watch for.
Why it happens
Rifampin induces CYP3A4 and CYP2C8, increasing enzalutamide clearance.
What to do
Use an alternative with little or no CYP induction when possible. If unavoidable, enzalutamide labeling advises increasing the daily dose from 160 mg to 240 mg, returning to the usual dose after the inducer is stopped.
What to ask your pharmacist
- Does the benefit of taking both outweigh the risk in my case?
- Do I need any blood test, ECG or other check while on both?
- What early warning signs should I watch for, and what should I do if they appear?
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References
Other interactions of Enzalutamide
- Doravirine + Enzalutamide Contraindicated
- Elbasvir / grazoprevir + Enzalutamide Contraindicated
- Ensitrelvir + Enzalutamide Contraindicated
- Enzalutamide + Fostemsavir Contraindicated
- Enzalutamide + Isavuconazonium Contraindicated
- Enzalutamide + Lenacapavir Contraindicated
Frequently asked questions
Can I take Enzalutamide with Rifampin?
MediHelp rates the interaction as major. Enzalutamide and Rifampin can interact in a way that may be serious. Using them together is sometimes necessary, but it needs a deliberate decision by the prescriber, a plan for monitoring, and clear advice on the warning signs to watch for. Rifampin is a strong CYP3A4 and CYP2C8 inducer and can lower enzalutamide and active metabolite exposure. This may reduce the clinical efficacy of prostate cancer therapy.
How serious is the interaction between Enzalutamide and Rifampin?
MediHelp rates it major, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Use an alternative with little or no CYP induction when possible. If unavoidable, enzalutamide labeling advises increasing the daily dose from 160 mg to 240 mg, returning to the usual dose after the inducer is stopped.
What other medicines interact with Enzalutamide?
MediHelp also lists interactions of Enzalutamide with, for example, Doravirine, Elbasvir / grazoprevir, Ensitrelvir. The full list is on the Enzalutamide page.
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