Drug interactions
Itraconazole + Regorafenib
Severity: Major
Itraconazole and Regorafenib: major interaction.
Last updated Sources: US FDA label
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 raises regorafenib parent drug levels while lowering its active metabolites, so the net effect on safety and efficacy is uncertain. Higher exposure of the parent drug may worsen hepatotoxicity and other adverse reactions.
What this interaction means in plain words
Itraconazole and Regorafenib 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; Regorafenib belongs to Oncology.
Why it happens
Strong CYP3A4 inhibition reduces conversion of regorafenib to its active metabolites M-2 and M-5 and increases parent drug exposure.
What to do
Avoid strong CYP3A4 inhibitors during regorafenib treatment and for a period after stopping them. Choose an alternative antifungal and monitor liver tests if exposure occurs.
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 Regorafenib
Frequently asked questions
Can I take Itraconazole with Regorafenib?
MediHelp rates the interaction as major. Itraconazole and Regorafenib 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 raises regorafenib parent drug levels while lowering its active metabolites, so the net effect on safety and efficacy is uncertain. Higher exposure of the parent drug may worsen hepatotoxicity and other adverse reactions.
How serious is the interaction between Itraconazole and Regorafenib?
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 strong CYP3A4 inhibitors during regorafenib treatment and for a period after stopping them. Choose an alternative antifungal and monitor liver tests if exposure occurs.
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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