Second-generation systemic triazole antifungal
ATC code: J02AC05 (Isavuconazole)
Brand names
Cresemba
Inhibits fungal 14-alpha-demethylase (CYP51) – blocks ergosterol synthesis. Active against Aspergillus, Mucorales and some rare fungi. Metabolised by CYP3A4 + CYP3A5; itself inhibits CYP3A4 (weaker than voriconazole and posaconazole) but uniquely SHORTENS QT, making it preferred when QT prolongation is a concern.
First line
Isavuconazole is first-line antifungal for invasive aspergillosis and mucormycosis. 2024 places it on par with voriconazole, preferring isavuconazole in patients at QT risk (methadone, ) and in renal impairment (the IV formulation is cyclodextrin-free).
4 pairs found. Sorted from critical to minor.
Mechanism
Carbamazepine is a strong CYP3A4 inducer. Isavuconazole falls significantly. Cresemba Section 4.3.
Symptoms
Mycosis progression.
Management
Combination contraindicated.
Mechanism
Strong CYP3A4 induction.
Symptoms
Mycosis progression.
Management
Combination contraindicated.
Mechanism
Rifampicin is a strong CYP3A4 inducer. Isavuconazole falls 97% – antifungal effect lost.
Symptoms
Fungal infection progression.
Management
Combination contraindicated. Cresemba Section 4.3.
Mechanism
Isavuconazole is a moderate CYP3A4 inhibitor. Sirolimus rises 1.5-2 fold.
Symptoms
Nephrotoxicity.
Management
Reduce sirolimus by 50% with blood level monitoring.
Opens the checker prefilled with this drug. Pick the second one from your regimen.
Limited data. EMA recommends only when necessary.
Breastfeeding not recommended.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Isavuconazole is evaluated for the following indications with varying evidence strength: Invasive aspergillosis (evidence tier A). See the full indication matrix with dosing and citations above on this page.
Common side effects of Isavuconazole (≥ 1 in 100): Nausea, vomiting, diarrhoea, Headache, Liver transaminase rise, Hypokalaemia. See the Safety section for uncommon and serious reactions.
FDA category C. Limited data. EMA recommends only when necessary.
Breastfeeding not recommended.
Isavuconazole is contraindicated in: Strong CYP3A4 inducers (rifampicin, phenytoin, carbamazepine); Strong CYP3A4 inhibitors (ketoconazole, high-dose ritonavir); Familial short QT syndrome. Full list in the Safety section.