Drug interactions
Lomitapide + Zileuton
Severity: Major
Lomitapide and Zileuton: major interaction.
Last updated
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
Lomitapide is a sensitive CYP3A4 substrate that causes dose-dependent hepatotoxicity and gastrointestinal effects. Zileuton, a weak CYP3A4 inhibitor, can raise lomitapide exposure, and zileuton also carries its own hepatotoxicity risk.
What this interaction means in plain words
Lomitapide and Zileuton 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.
Lomitapide belongs to Cardiovascular; Zileuton belongs to Respiratory.
Why it happens
Zileuton inhibits CYP3A4, reducing first-pass and systemic metabolism of lomitapide.
What to do
Limit the lomitapide dose to no more than 30 mg daily when used with weak CYP3A4 inhibitors, and monitor ALT and bilirubin closely. Consider an alternative to zileuton if feasible.
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?
Pro+ members
Unlock the full page
Create an account and start a Pro+ trial to unlock the full management advice for Lomitapide and Zileuton, the additional notes, the evidence detail and the whole-prescription interaction checker.
- Full clinical management advice
- Additional notes
- Evidence detail
- Interaction checker for a whole prescription
Try Pro+ free for 14 days on the web. No card needed.
Other interactions of Zileuton
- Fezolinetant + Zileuton Contraindicated
- Pimozide + Zileuton Contraindicated
- Alosetron + Zileuton Major
- Clozapine + Zileuton Major
- Lonafarnib + Zileuton Major
- Theophylline + Zileuton Major
Other interactions of Lomitapide
- Aprepitant + Lomitapide Contraindicated
- Clarithromycin + Lomitapide Contraindicated
- Crizotinib + Lomitapide Contraindicated
- Diltiazem + Lomitapide Contraindicated
- Efavirenz + Lomitapide Contraindicated
- Ensitrelvir + Lomitapide Contraindicated
Frequently asked questions
Can I take Lomitapide with Zileuton?
MediHelp rates the interaction as major. Lomitapide and Zileuton 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. Lomitapide is a sensitive CYP3A4 substrate that causes dose-dependent hepatotoxicity and gastrointestinal effects. Zileuton, a weak CYP3A4 inhibitor, can raise lomitapide exposure, and zileuton also carries its own hepatotoxicity risk.
How serious is the interaction between Lomitapide and Zileuton?
MediHelp rates it major, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Limit the lomitapide dose to no more than 30 mg daily when used with weak CYP3A4 inhibitors, and monitor ALT and bilirubin closely. Consider an alternative to zileuton if feasible.
What other medicines interact with Zileuton?
MediHelp also lists interactions of Zileuton with, for example, Fezolinetant, Pimozide, Alosetron. The full list is on the Zileuton page.
Full monographs, dosing and an interaction checker in the MediHelp app
Open the complete reference, check multi-drug interactions and use dosing tools in the MediHelp app.
