Isavuconazole

Isavuconazole (BAL-4815) is a triazole prodrug with antifungal activity against yeasts, molds, and dimorphic fungi. Isavuconazole inhibits ergosterol biosynthesis and results in the disruption of fungal membrane structure and function. Isavuconazole is a moderate inhibitor of CYP3A4. In Vitro: Isavuconazole (BAL-4815) shows good activity against all Candida spp., with active MIC₅₀ of 0.004 mg/L. The MIC₅₀s/MIC₉₀s range from 0.002/0.004 mg/L for C. albicans to 0.25/0.5 mg/L for C. glabrata^[1]. Isavuconazole has potent in vitro activity against most common Aspergillus species, Purpureocillium lilacinum, and Scedosporium apiospermum^[2]. Isavuconazole shows potent activity against molds, yeasts, and dimorphic fungi. Rhizopus isolates have MIC values to isavuconazole as low as 0.12 µg/mL with others as high as 32 µg/mL^[3]. In the study of pharmacokinetics and pharmacodynamics of isavuconazole against the GFP transformant, F/11628, NIH 4215, and F/16216, the modal MICs of isavuconazole are 1, 8, 1, 4 mg/L, respectively^[4].