VORICONAZOLE

VORICONAZOLE

PRODUCT IDENTIFICATION

CAS NO.

137234-62-9

VORICONAZOLE

EINECS NO.

FORMULA

C₁₆H₁₄F₃N₅O

MOL WT.

349.32

H.S. CODE

TOXICITY

SYNONYMS

Vfend

(2R, 3S)-2-(2,4-difluorophenyl)-3-(5-fluoro-4- pyrimidinyl)-1-(1H-1,2,4-triazol-1- yl)-2-butanol; (alphaR, betaS)-alpha-(2,4-difluorophenyl)-5-fluoro-beta-methyl-alpha- (1H-1,2,4-triazol-1- ylmethyl)-4-pyrimidineethanol;

SMILES

CLASSIFICATION

PHYSICAL AND CHEMICAL PROPERTIES

PHYSICAL STATE

white to off white crystalline powder

MELTING POINT

127 - 130 C

BOILING POINT

SPECIFIC GRAVITY

SOLUBILITY IN WATER

SOLVENT SOLUBILITY

VAPOR DENSITY

REFRACTIVE INDEX

AUTOIGNITION

NFPA RATINGS

FLASH POINT

STABILITY

Stable under ordinary conditions

GENERAL DESCRIPTION & EXTERNAL LINKS

Voriconazole is a triazole class antifungal agent used as a fungicidal against Aspergillus and fungistatic against Candida especially. Voriconazole is structurally related to fluconazole. Like all azole antifungal agents, voriconazole works principally via inhibition of fungal-cytochrome P-450-14alpha--demethylase which leads to an accumulation of 14 alpha-methyl sterols, resulting in the loss of ergosterol in the cell wall. Compared to fluconazole, voriconazole inhibits the enzyme to a greater extend. Voriconazole is a white to off-white crystalline powder; melting point 127 C; administered orally or intravenously. Chemical designation is (2R, 3S)-2-(2,4-difluorophenyl)-3-(5-fluoro-4- pyrimidinyl)-1-(1H-1,2,4- triazol-1- yl)-2-butanol.

Voriconazole: the newest triazole antifungal agent........INDICATIONS Voriconazole (VFEND, Pfizer Ireland Pharmaceuticals, Ringaskiddy, Ireland) is a triazole antifungal agent that inhibits fungal ergosterol biosynthesis (5). It is structurally related to fluconazole, with the major difference being the substitution of a fluoropyrimidine grouping in place of a triazole moiety (5, 6). Voriconazole is indicated for the treatment of invasive aspergillosis. It is also indicated for the treatment of fungal infections caused by S. apiospermum or Fusarium spp. that are refractory to other antifungal agents (5). PHARMACOLOGY Like the other triazole antifungals, voriconazole exerts its antifungal activity by inhibition of 14-alpha-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes (2, 5, 6). This inhibition is more selective for fungal than for mammalian enzyme systems. The accumulation of 14-alphamethyl sterols results in a decrease in ergosterol, which is an essential component of fungal cell wall formation. The resulting cell wall abnormalities are thought to be responsible for voriconazole��s antifungal activity.........(http://www.baylorhealth.edu/)

SALES SPECIFICATION

APPEARANCE

white to off white crystalline powder

ASSAY

99.0% min

MELTING POINT

129 C - 132 C

SPECIFIC ROTATION

-54° ~ -59°

FLUORIDE CONTENT

14.7 - 17.9%

OPTICAL ISOMER

0.1% max

RELATED SUBSTANCES

0.5% max (total), 0.1% max (Individual)

TRANSPORTATION

PACKING

HAZARD CLASS

UN NO.

PRICE INFORMATION