Isavuconazonium sulfate

Isavuconazonium sulfate is a broad spectrum antifungal agent that was codeveloped by Basilea Pharmaceutica (a subsidiary of Hoffmann-La Roche acquired in 2000) and Astellas Pharma, which obtained its first approval by the United States Food and Drug Administration (FDA) for the treatment of invasive aspergillosis and invasive mucormycosis, available as both oral and intravenous formulations. Isavuconazonium sulfate is a water-soluble prodrug, which is rapidly hydrolyzed by esterases (mainly butylcholinesterase) in plasma into the active moiety isavuconazole (BAL-4815) and an inactive cleavage product (BAL-8728). Isavuconazole inhibits cytochrome P450 (CYP)- dependent enzyme lanosterol 14-ademethylase (CYP51) and thereby inhibits the synthesis of ergosterol, a key component of the fungal cell membrane.4 Isavuconazole displayed potent fungistatic or fungicidal activity in vitro against a broad range of clinically important yeasts and molds, namely Candida spp., Cryptococcus spp., Trichosporon spp., Geotrichum capitatum, Pichia spp., Rhodotorula spp., Saccharomyces cerevisiae, Aspergillus spp., and most species known to cause mucormycosis (Mucorales mucorales). This broad range of antifungal activity renders this drug more clinically appealing compared to other azoles with narrower indications. Furthermore, isavuconazole does not require a cyclodextrin vehicle due to its water solubility, and currently does not require therapeutic drug monitoring. Moreover, isavuconazole has displayed improved safety and tolerability compared to voriconazole.

ChEBI: Isavuconazonium is an organic cation that is the cationic portion of isavuconazonium sulfate (a prodrug for isavuconazole, an antifungal agent used for the treatment of invasive aspergillosis and invasive mucormycosis). It has a role as a prodrug, an ergosterol biosynthesis inhibitor, an EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor and an antifungal agent.

Isavuconazonium Sulfate can be prepared to be used as an antifungal drug.