Lomitapide and Ketoconazole Topical: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Lomitapide
No brand names on recordKetoconazole Topical
How we grade severity & evidence
Severity levels
- Contraindicated: These should generally not be used together.
- Major: Potentially serious — often needs a change or close monitoring.
- Moderate: Can be significant — usually manageable with monitoring.
- Minor: Usually limited clinical impact.
Evidence grades
- Established: Well documented — supported by controlled studies or strong clinical data.
- Probable: Good supporting evidence, though not definitively proven.
- Suspected: Some evidence suggests this interaction, but it is not well established.
- Possible: Limited or conflicting evidence; the interaction may occur.
- Theoretical: Predicted from the drugs' pharmacology; not yet confirmed in people.
Ratings come from the documented interaction literature and are reviewed by a pharmacist. They describe the documented risk of the combination, not what will necessarily happen to you — your dose, timing, and health picture all matter.
What happens
Increased lomitapide exposure
Interaction Deep Dive
Concomitant use of lomitapide (a CYP3A4 substrate) with a strong CYP3A4 inhibitor is contraindicated, as coadministration may result in increased exposure of lomitapide. In a study with concomitant use of a strong CYP3A4 inhibitor (ketoconazole 200 mg twice daily for 9 days) and lomitapide (60 mg daily), lomitapide AUC was increased by 27-fold and Cmax was increased by 15-fold. One patient had markedly elevated transaminases (ie, ALT and AST) within days of initiating clarithromycin, a strong CYP3A4 inhibitor, during lomitapide clinical trials. If treatment with a strong CYP3A4 inhibitor is unavoidable, discontinue lomitapide during the course of treatment1.
Why it happens (mechanism)
Inhibition of CYP3A4-mediated metabolism of lomitapide
Literature reports
2 reports — tap to read
a) During lomitapide clinical trials, a patient with homozygous familial hypercholesterolemia (HoFH) had markedly elevated transaminases (ALT, 24 times ULN; AST, 13 times ULN) within days of initiating clarithromycin, a strong CYP3A4 inhibitor 1.
b) In a drug interaction study, concomitant use of a strong CYP3A4 inhibitor (ketoconazole 200 mg twice daily for 9 days) and lomitapide (60 mg daily) increased lomitapide AUC and Cmax by 27-fold and by 15-fold, respectively 1.
Common questions
Can I take Lomitapide and Ketoconazole Topical together?
Increased lomitapide exposure Always confirm with your pharmacist or prescriber before making any change.
How serious is the Lomitapide and Ketoconazole Topical interaction?
It is rated contraindicated. These should generally not be used together.
How quickly could this interaction happen?
The documented onset is "unspecified". The timing of this interaction is not well characterized.
How strong is the evidence for this interaction?
The evidence is graded "probable". Good supporting evidence, though not definitively proven.
Questions for your pharmacist
- Does my dose of Lomitapide or Ketoconazole Topical need adjusting while I take them together?
- What symptoms should prompt me to call you or my prescriber right away?
- Does the timing of my doses matter for this combination?
- Is there a safer alternative to one of these medications for me?
References (1)
- Product Information: JUXTAPID® oral capsules, lomitapide oral capsules. Chiesi USA, Inc. (per Manufacturer), Cary, NC, 2026. DailyMed
Keep reading about Lomitapide
Keep reading about Ketoconazole Topical
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