Voriconazole

Voriconazole is a triazole antifungal medication that is generally used to treat serious, invasive fungal infections. Voriconazole has also been proven effective against a number of other serious fungal pathogens. This includes infections by Fusarium spp and Scedosporium apiospermum (asexual form of Pseudallescheria boydii). Although infrequently seen, these molds are emerging as more common and deadly causes of fungal infection in seriously immunocompromised patients, and the development of voriconazole has been an important advance in their treatment as they are generally resistant to other antifungal agents (including amphotericin B). Voriconazole is the first and only drug ever specifically indicated for their treatment by the FDA. Voriconazole has also been used to treat severe fungal corneal infection.

Product information

CAS Number: 137234-62-9

Molecular Weight: 349.31

Formula: C16H14F3N5O

Synonym:

UK-109496

UK 109496

UK109496

Vfend

UK109, 496

UK-109, 496

UK 109, 496

Chemical Name: (2R, 3S)-2-(2, 4-Difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1, 2, 4-triazol-1-yl)butan-2-ol

Smiles: C[C@@H](C1=NC=NC=C1F)[C@](O)(CN1C=NC=N1)C1=CC=C(F)C=C1F

InChiKey: BCEHBSKCWLPMDN-MGPLVRAMSA-N

InChi: InChI=1S/C16H14F3N5O/c1-10(15-14(19)5-20-7-22-15)16(25,6-24-9-21-8-23-24)12-3-2-11(17)4-13(12)18/h2-5,7-10,25H,6H2,1H3/t10-,16+/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 70 mg/mL(200.39 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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.

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.

References:

1. Kirkpatrick WR, et al. Antimicrob Agents Chemother, 2002, 46(8), 2564-2568.
2. Diekema DJ, et al. J Clin Microbiol, 2003, 41(8), 3623-3626.
3. Espinel-Ingroff A, et al. J Clin Microbiol, 1998, 36(1), 198-202.

Products are for research use only. Not for human use.