Voriconazole-d3

Voriconazole-d3 is an Ergosterol biosynthesis inhibitor and a labeled form of Voriconazole. This mono triazole antifungal agent inhibits the growth of Candida, Cryptococcus, and Aspergillus species. Studies suggest that Voriconazole-d3 can be synthesized by modifying the structure of fluconazole. This antifungal agent functions by inhibiting cytochrome P450 dependent 14-α-sterol demethylase, which is responsible for the biosynthesis of Ergosterol. Furthermore, Voriconazole-d3 inhibits fungal growth, cell wall thinning, and cell membrane degradation.

Voriconazole is a triazole antifungal agent used primarily in the treatment or prevention of aspergillosis and candidal infections. However, its therapy may cause transient, asymptomatic serum aminotransferase elevations, and it is also a well-known cause of acute drug-induced liver injury.

Voriconazole-d3 is derived from 2,4-Difluoro-α-(1H-1,2,4-triazolyl)acetophenone, which is an antifungal activity, particularly toward Candida albicans and Candida parapsilosis.

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Belanger, P., et al. 1997. Antimicrob. Agents Chemother. 41: 1840-1842. PMID: 9257776
2. In vitro activities of voriconazole (UK-109,496) and four other antifungal agents against 394 clinical isolates of Candida spp
Marco, F., et al. 1998. Antimicrob. Agents Chemother. 42: 161-163. PMID: 9449278
3. In vitro activity of the new triazole voriconazole (UK-109,496) against opportunistic filamentous and dimorphic fungi and common and emerging yeast pathogens
Espinel-Ingroff, A. 1998. J. Clin. Microbiol. 36: 198-202. PMID: 9431946