Isavuconazole: A Comprehensive Overview of a ...

Isavuconazole: A Comprehensive Overview of a Novel Broad-Spectrum Antifungal Agent

Author Name : Patane Pratiksha, Hindole Sunil, Gavhane Aanjali, Kore Pratiksha, Yogita Bhingole

ABSTRACT Isavuconazole, a broad-spectrum triazole antifungal medication, is administered as a prodrug, isavuconazonium sulfate (commercial name CRESEMBA), for treating invasive aspergillosis and mucormycosis in adults. Available in intravenous and oral formulations, isavuconazole inhibits ergosterol synthesis in fungal cell membranes, disrupting membrane function and causing fungal cell death. This azole demonstrates extensive antifungal activity, even against azole-resistant strains. Isavuconazole's pharmacokinetics are notable for high oral bioavailability (98%), minimal inter subject variability, and a long terminal half-life (100–130 hours). It undergoes rapid conversion from prodrug to active form, with maximum plasma concentrations reached within 2-3 hours post-oral administration. Unlike other azoles, it does not require solubilizing vehicles in its IV formulation, reducing potential nephrotoxicity. While isavuconazole has fewer drug interactions compared to voriconazole and posaconazole, it can still affect drugs metabolized by CYP3A4. Its pharmacokinetics are influenced by hepatic impairment but not significantly altered by renal impairment, age, or gender. The drug shows potential advantages over other triazoles, including linear kinetics, minimal interpatient variability, and no need for dietary adjustments for absorption. The current antifungal treatment landscape faces challenges, such as limited drug classes, cross-resistance, and a lack of new drug development. The emergence of multidrug-resistant fungal species underscores the need for novel therapeutics. Despite these challenges, isavuconazole's efficacy and safety profile position it as a valuable addition to antifungal therapy, particularly for invasive fungal infections where resistance to other agents is a concern.