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Drug interactions

Entrectinib + Imatinib

Severity: Major

Entrectinib and Imatinib: 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

Imatinib, a moderate CYP3A4 inhibitor, can increase entrectinib exposure. This raises the risk of QT prolongation, heart failure, cognitive effects and other dose-related toxicity.

What this interaction means in plain words

Entrectinib and Imatinib 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.

Entrectinib belongs to Oncology; Imatinib belongs to Oncology.

Evidence level: Moderate

Why it happens

Imatinib inhibits CYP3A4-mediated metabolism of entrectinib.

What to do

Avoid if possible. If it is required, reduce the entrectinib dose per labeling, monitor ECG and for neurologic and cardiac toxicity, and restore the dose 3-5 half-lives after imatinib 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?

Bring a full list of your medicines, including over-the-counter products, supplements and herbal remedies, to every pharmacy visit.

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Frequently asked questions

Can I take Entrectinib with Imatinib?

MediHelp rates the interaction as major. Entrectinib and Imatinib 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. Imatinib, a moderate CYP3A4 inhibitor, can increase entrectinib exposure. This raises the risk of QT prolongation, heart failure, cognitive effects and other dose-related toxicity.

How serious is the interaction between Entrectinib and Imatinib?

MediHelp rates it major, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Avoid if possible. If it is required, reduce the entrectinib dose per labeling, monitor ECG and for neurologic and cardiac toxicity, and restore the dose 3-5 half-lives after imatinib is stopped.

What other medicines interact with Imatinib?

MediHelp also lists interactions of Imatinib with, for example, Lomitapide, Lonafarnib, Amobarbital. The full list is on the Imatinib page.

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