Voriconazole-d₃  (Synonyms: UK-109496-d₃)

Voriconazole-d₃ is the deuterium labeled Voriconazole. Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes[1][2].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

352.33

C₁₆H₁₁D₃F₃N₅O

1217661-14-7

固体

White to off-white

伏立康唑 d₃

Room temperature in continental US; may vary elsewhere.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [2]. Nickie D Greer. Voriconazole: the newest triazole antifungal agent.Proc (Bayl Univ Med Cent). 2003 Apr;16(2):241-8.

  [3]. Lesley J Scott, et al. Voriconazole : a review of its use in the management of invasive fungal infections.Drugs. 2007;67(2):269-98.  [Content Brief]

  [4]. A M Sugar,et al. Efficacy of voriconazole in treatment of murine pulmonary blastomycosis.Antimicrob Agents Chemother. 2001 Feb;45(2):601-4.  [Content Brief]