Drug interactions
Itraconazole + Selumetinib
Severity: Major
Itraconazole and Selumetinib: major interaction.
Last updated Sources: UK SmPC
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
Itraconazole increases selumetinib exposure by inhibiting CYP3A4. This may worsen gastrointestinal, skin and cardiac toxicity including reduced ejection fraction.
What this interaction means in plain words
Itraconazole and Selumetinib 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.
Itraconazole belongs to Anti Fungals; Selumetinib belongs to Oncology.
Why it happens
Strong CYP3A4 inhibition reduces selumetinib clearance.
What to do
Avoid if possible. If unavoidable, reduce the selumetinib dose per labeling and resume the prior dose about three half-lives after stopping the inhibitor.
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?
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References
Other interactions of Itraconazole
- Alfuzosin + Itraconazole Contraindicated
- Alprazolam + Itraconazole Contraindicated
- Avanafil + Itraconazole Contraindicated
- Conivaptan + Itraconazole Contraindicated
- Dihydroergotamine intranasal + Itraconazole Contraindicated
- Dihydroergotamine + Itraconazole Contraindicated
Other interactions of Selumetinib
Frequently asked questions
Can I take Itraconazole with Selumetinib?
MediHelp rates the interaction as major. Itraconazole and Selumetinib 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. Itraconazole increases selumetinib exposure by inhibiting CYP3A4. This may worsen gastrointestinal, skin and cardiac toxicity including reduced ejection fraction.
How serious is the interaction between Itraconazole and Selumetinib?
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 unavoidable, reduce the selumetinib dose per labeling and resume the prior dose about three half-lives after stopping the inhibitor.
What other medicines interact with Itraconazole?
MediHelp also lists interactions of Itraconazole with, for example, Alfuzosin, Alprazolam, Avanafil. The full list is on the Itraconazole page.
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