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Drug interactions

Entrectinib + Fluconazole

Severity: Major

Entrectinib and Fluconazole: 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

Fluconazole can raise entrectinib concentrations through CYP3A4 inhibition, while both drugs also prolong the QT interval. Together this increases the risk of entrectinib toxicity and torsades de pointes.

What this interaction means in plain words

Entrectinib and Fluconazole 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; Fluconazole belongs to Anti Fungals.

Evidence level: Moderate

Why it happens

CYP3A4 inhibition raising entrectinib exposure, plus additive QT prolongation.

What to do

Avoid the combination if possible. If necessary, reduce entrectinib dose per labeling (200 mg/day for adults with BSA above 1.50 m2), monitor ECG and electrolytes, and restore the dose after 3-5 half-lives of stopping fluconazole.

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 Fluconazole?

MediHelp rates the interaction as major. Entrectinib and Fluconazole 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. Fluconazole can raise entrectinib concentrations through CYP3A4 inhibition, while both drugs also prolong the QT interval. Together this increases the risk of entrectinib toxicity and torsades de pointes.

How serious is the interaction between Entrectinib and Fluconazole?

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 the combination if possible. If necessary, reduce entrectinib dose per labeling (200 mg/day for adults with BSA above 1.50 m2), monitor ECG and electrolytes, and restore the dose after 3-5 half-lives of stopping fluconazole.

What other medicines interact with Fluconazole?

MediHelp also lists interactions of Fluconazole with, for example, Dihydroergotamine intranasal, Dihydroergotamine, Dofetilide. The full list is on the Fluconazole page.

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