Drug intelligence / Profile preview

isavuconazonium

Development stage
Approved
Lead developer
Basilea Pharmaceutica
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

Isavuconazonium is a second-generation triazole antifungal used to treat serious fungal infections, specifically invasive aspergillosis and invasive mucormycosis in adults and children. It acts as a prodrug of isavuconazole, which inhibits the synthesis of ergosterol—a key component of the fungal cell membrane—by blocking the cytochrome P-450-dependent enzyme lanosterol 14-alpha-demethylase (CYP51). This disruption weakens the fungal cell membrane, leading to cell death. Isavuconazonium offers high water solubility for intravenous use and good oral bioavailability. It was developed as an alternative to other azole antifungals that require cyclodextrin for IV administration, thus reducing nephrotoxicity risk. The drug was approved by the FDA in 2015 and marketed under the brand name Cresemba[1][2][3][5][6].

Brand names
Cresemba
Other names
isavuconazonium sulfateisavuconazole prodrug
02

Targets

CYP51A1 (Sterol 14α-demethylase)KCNH2 (Voltage-gated potassium channel subfamily H member 2)

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