product name Voriconazole
Description: Voriconazole is a novel triazole antifungal medication similar to fluconazole and itraconazole that acts by inhibiting fungal cytochrome P-450-dependent, 14-alpha-sterol demethylase-mediated synthesis of ergosterol. Voriconazole is used to treat serious, invasive fungal infections. Voriconazole has also been proven effective against a number of other serious fungal pathogens including infections by Fusarium spp and Scedosporium apiospermum.
References: J Clin Microbiol. 1998 Jan;36(1):198-202; J Clin Microbiol. 2003 Aug;41(8):3623-6; Antimicrob Agents Chemother. 2002 Aug;46(8):2564-8.
349.31
Formula
C16H14F3N5O
CAS No.
137234-62-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 70 mg/mL (200.4 mM)
Water: <1 mg/mL
Ethanol: 20 mg/mL (57.3 mM)
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% propylene glycol: 10mg/mL
Synonyms
UK-109496
other peoduct :
| In Vitro |
In vitro activity: Voriconazole is active against certain opportunistic filamentous and dimorphic fungi (molds) and yeasts. Voriconazole in vitro activities are higher than or similar to those of itraconazole and amphotericin B for most of the molds tested, with the exceptions of R. arrhizus and S. schenckii. Voriconazole inhibits 95% of isolates at ≤1 μg/ml against 448 recent clinical mold isolates Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Voriconazole is significantly more effective than itraconazole in reducing Aspergillus content in the lungs of immunocompromised guinea pig with pulmonary aspergillosis. Voriconazole also has been shown to be effective in guinea pigs with experimental pulmonary or intracranial infections caused by C. neoformans. Voriconazole (5 mg/kg/day, i.p.) combined with Amphotericin B (1.25 mg/kg/day, i.p.) significantly reduces the colony counts in the tissues of selected Guinea pigs compared with those in the tissues of the controls. Voriconazole (5 mg/kg/day, i.p.) combined with Amphotericin B (1.25 mg/kg/day, i.p.) also results in reductions in colony counts in tissues compared with those in the tissues of Guinea pigs treated with caspofungin acetate (the difference is not statistically significant) and improves the survival times but does not sterilize tissues. Voriconazole (5 mg/kg/day, i.p.) combined with caspofungin acetate (CAS) at either dose reduces colony counts in tissues 1,000-fold over those for the controls and are the only regimens that significantly reduces the numbers of positive cultures. |
| Animal model | |
| Formulation & Dosage | |
| References | J Clin Microbiol. 1998 Jan;36(1):198-202; J Clin Microbiol. 2003 Aug;41(8):3623-6; Antimicrob Agents Chemother. 2002 Aug;46(8):2564-8. |
