MajorAntifungal, triazole×Selective immunosuppressant, mTOR inhibitor
Updated · Methodology
Mechanism
Itraconazole is a strong inhibitor of CYP3A4 and P-glycoprotein, and sirolimus is cleared through both. The pair has not been studied directly: the itraconazole SmPC says a rise in sirolimus levels is likely and does not recommend the combination. The sirolimus SmPC and the FDA label also advise against strong CYP3A4 inhibitors and name itraconazole. No label lists the pair as a contraindication.
Symptoms
Acute nephrotoxicity, hepatotoxicity, cytopenia.
Management
Avoid the combination during itraconazole therapy and for 2 weeks after it, as the itraconazole SmPC and the FDA label state. For a fungal infection in a patient on sirolimus, the FDA sirolimus label advises an antifungal with lower interaction potential. If itraconazole is still needed, measure sirolimus blood levels more often and reduce or pause the dose according to the result.
Check the full regimen, not just this pair
Opens the checker with these two drugs prefilled. Add the rest of the regimen and recompute additive risks.
Summary of a multi-drug list →
Medicine list: everything you take in one place →
Sources
- FDA: Sporanox (itraconazole) capsules prescribing information (2026)– Janssen Pharmaceuticals. SPORANOX (itraconazole) capsules. Prescribing information, DailyMed setid a4d555fa-787c-40fb-bb7d-b0d4f7318fd0, Contraindications and Drug Interactions table
- FDA: Sirolimus tablet (Northstar Rx LLC) – Prescribing Information – strong CYP3A4 inhibitor contraindications (2020)– FDA Rapamune label, Drug Interactions §7.2; DailyMed setid ad39eb60-1fa0-4722-8ba1-523194921c2a
- FDA: Rapamune (sirolimus) prescribing information (2017)
- AEMPS: Ficha técnica Sporanox 100 mg cápsulas (itraconazol) (2026)– AEMPS CIMA, Sporanox 100 mg cápsulas, nº registro 59343, secciones 4.3 y 4.5
- EMA: Rapamune (sirolimus) – ficha técnica en CIMA (2026)– AEMPS CIMA, Rapamune 1 mg comprimidos recubiertos, nº registro 01171008 (EU/1/01/171), secciones 4.3, 4.4 y 4.5
- FDA: Sirolimus tablets prescribing information (Mylan) (2026)– Mylan Pharmaceuticals. Sirolimus tablets. Prescribing information, DailyMed setid 5908cd1a-fc5a-462f-99ed-1d8983e253c9, sections 4, 5.20 and 7.2 (Rapamune itself is no longer listed on DailyMed)