Irinotecan and Ketoconazole: Drug Interaction Guide
Quick answer: This is a major interaction — avoid combining Irinotecan and Ketoconazole unless specifically directed by your doctor.
How Irinotecan interacts with Ketoconazole
Ketoconazole inhibits CYP3A4 and UGT1A1, increasing exposure to irinotecan's active metabolite SN-38 with severe neutropenia and diarrhea.
What you should do
Avoid azole antifungals during irinotecan therapy; use micafungin or amphotericin B if antifungal coverage is needed.
Key facts
Severity
Major — avoid combination
Mechanism
Ketoconazole inhibits CYP3A4 and UGT1A1, increasing exposure to irinotecan's active metabolite SN-38 with severe neutrop...
Action
Avoid azole antifungals during irinotecan therapy; use micafungin or amphotericin B if antifungal coverage is needed.
Frequently asked questions
Can I take Irinotecan and Ketoconazole together?
No — this combination should generally be avoided. Avoid azole antifungals during irinotecan therapy; use micafungin or amphotericin B if antifungal coverage is needed.
What is the severity of this interaction?
The interaction between Irinotecan and Ketoconazole is classified as Major — avoid combination. Ketoconazole inhibits CYP3A4 and UGT1A1, increasing exposure to irinotecan's active metabolite SN-38 with severe neutropenia and diarrhea.
What should I do if I'm prescribed both?
Avoid azole antifungals during irinotecan therapy; use micafungin or amphotericin B if antifungal coverage is needed. Always consult your prescribing clinician — do not stop or change medications without medical guidance.
Last reviewed: by iMedic Medical Editorial Team. Our editorial process.