Entrectinib and Lumefantrine: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Lumefantrine
No brand names on recordEntrectinib
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 artemether/lumefantrine exposure and an increased risk of QT prolongation
Interaction Deep Dive
Avoid concomitant use of drugs that prolong the QTc or QT interval, such as artemether/lumefantrine as it may add to the QTc or QT effects of entrectinib and increase the risk of cardiac arrhythmias. If concomitant use cannot be avoided, assess QT interval and electrolytes prior to initiation of entrectinib and periodically during treatment. Based on the severity of QTc interval prolongation, withhold entrectinib and then resume at same or reduced dose, or permanently discontinue1. Coadministration of artemether/lumefantrine and entrectinib (CYP3A4 inhibitor) may also increase artemether/lumefantrine exposure. If concomitant administration of artemether/lumefantrine and QT prolonging agent is medically required, monitor the ECG. Additionally, caution is advised when administering drugs that prolong the QT interval after completing artemether/lumefantrine therapy due to the long half-life of lumefantrine (3 to 6 days) 2.
Why it happens (mechanism)
Inhibition of CYP3A4-mediated metabolism of artemether/lumefantrine; additive QT interval prolongation
Common questions
Can I take Entrectinib and Lumefantrine together?
Increased artemether/lumefantrine exposure and an increased risk of QT prolongation Always confirm with your pharmacist or prescriber before making any change.
How serious is the Entrectinib and Lumefantrine interaction?
It is rated major. Potentially serious — often needs a change or close monitoring.
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 "theoretical". Predicted from the drugs' pharmacology; not yet confirmed in people.
Questions for your pharmacist
- Does my dose of Entrectinib or Lumefantrine 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 (2)
- Product Information: ROZLYTREK(R) oral capsules, pellets, entrectinib oral capsules, pellets. Genentech Inc (per FDA), South San Francisco, CA, 2023. DailyMed
- Product Information: COARTEM® oral tablets, artemether lumefantrine oral tablets. Novartis Pharmaceuticals Corporation (per DailyMed), East Hanover, NJ, 2025. DailyMed
Keep reading about Lumefantrine
Keep reading about Entrectinib
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