Voriconazole-d3 (Synonyms: VRC-d3)

Voriconazole-d₃ is intended for use as an internal standard for the quantification of voriconazole by GC- or LC-MS. Voriconazole is a triazole antifungal agent and a derivative of fluconazole .^1,2 It is active against a variety of yeast and fungi, including clinical isolates of A. flavus, A. fumigatus, F. oxysporum, F. solani, C. albicans, and C. neoformans (MICs = <0.03-16 µg/ml).¹ Voriconazole is also active against 56 clinical isolates of fluconazole-resistant C. albicans (MICs = 0.015-8 µg/ml).² It inhibits ergosterol biosynthesis in C. albicans, C. glabrata, A. fumigatus, and A. flavus (IC₅₀s = 0.03-1 µg/ml).³ Voriconazole (10 mg/kg twice per day, i.v.) decreases the number of lung colony-forming units (CFUs), reduces alveolar collapse and lung inflammatory cell infiltration and necrosis, and increases survival in a rat model of invasive pulmonary aspergillosis.⁴ Formulations containing voriconazole have been used in the treatment of fungal infections.

1.Espinel-Ingroff, A.In vitro activity of the new triazole voriconazole (UK-109,496) against opportunistic filamentous and dimorphic fungi and common and emerging yeast pathogensJ. Clin. Microbiol.36(1)198-202(1998) 2.Cuenca-Estrella, M., DÍaz-Guerra, T.M., Mellado, E., et al.Comparative in vitro activity of voriconazole and itraconazole against fluconazole-susceptible and fluconazole-resistant clinical isolates of Candida species from SpainEur. J. Clin. Microbiol. Infect. Dis.18(6)432-435(1999) 3.Munayyer, H.K., Mann, P.A., Chau, A.S., et al.Posaconazole is a potent inhibitor of sterol 14α-demethylation in yeasts and moldsAntimicrob. Agents Chemother.48(10)3690-3696(2004) 4.Zhang, M., Su, X., Sun, W.-K., et al.Efficacy of the combination of voriconazole and caspofungin in experimental pulmonary aspergillosis by different Aspergillus speciesMycopathologia177(1-2)11-18(2014)