Isavuconazonium sulfate

Antifungal

-20

Isavuconazonium sulfate is hydrolyzed by plasma esterases to yield the active moiety isavuconazole. Isavuconazole binds to and inhibits the fungal cytochrome P450 family enzyme lanosterol 14-alpha-demethylase (CYP51), which catalyzes the demethylation of lanosterol to yield ergosterol, an important component of the fungal cell membrane. Isavuconazonium Sulfate is a prodrug of the triazole antifungal agent isavuconazole, with broad-spectrum antifungal activity. Inhibition of CYP51 leads to a decrease in fungal ergosterol production and disrupts the synthesis of the fungal cell membrane, which decreases membrane integrity, increases cell membrane permeability and promotes the loss of essential intracellular elements. This results in fungal cell lysis and death.

Isavuconazole (BAL4815; trade name Cresemba) is a triazole antifungal drug. Isavuconazole has been approved by the FDA for treatment of invasive aspergillosis and invasive mucormycosis in adults. Both infections are caused by mold and fungi common to the environment, and occur in individuals who are immunosuppressed or have other complicating conditions, such as diabetes or lung disease