Isavuconazole is an Azol antifungal belonging to the triazole class and has broad-spectrum antifungal activity. It was discovered in Kamakura, Japan (Roche). The compound exhibits antifungal activity against bacteria causing invasive aspergillosis (Aspergillus flavus, Aspergillus fumigatus, and Aspergillus niger). Isavuconazole is also effective against Mucorales (the causative agent of mucormycosis) and Mucormycetes.
| Mechanism of Action | Isavuconazole disrupts the biosynthesis of ergosterol, which is a key component of the fungal cell membrane. It inhibits the cytochrome P450-dependent enzyme lanosterol 14-alpha-demethylase, that mediates the conversion of lanosterol to ergosterol. Depletion of ergosterol within the fungal cell membrane leads to decreased structural integrity and function of the cell membrane. |
| Microbiology Applications |
Isavuconazonium sulfate is the prodrug of the azole antifungal isavuconazole. Isavuconazole is a broad-spectrum antifungal with an in vitro activity profile similar to that of voriconazole, but with the additional advantage of having activity against the members of the order Mucorales such as Lichtheimia, Rhizopus, and Rhizomucor spp. Dimorphic fungi are unique and can exist in two different forms (as a mold or yeast) depending on environmental conditions. Dimorphic fungi may cause blastomycosis, coccidioidomycosis, emergomycosis, histoplasmosis, paracoccidioidomycosis, sporotrichosis, and talaromycosis and represent a diverse group. |
| Spectrum | Broad-spectrum with activity against yeasts (most Candida species.) molds (most Aspergillus species), and dimorphic fungi. |
| Molecular Formula | C22H17F2N5OS |
| References |
Miceli MH and Kauffman CA (2015) Isavuconazole: A new broad-spectrum triazole antifungal agent. Clin. Infect. Dis. 61 (10):1558–1565 PMID 26179012 2022) New perspectives on antimicrobial agents: Isavuconazole. Antimicrob. Agents Chemother. 66:e00177-22 |