Isavuconazole

Modify Date: 2024-01-05 11:18:14

Isavuconazole Structure
Isavuconazole structure
Common Name Isavuconazole
CAS Number 241479-67-4 Molecular Weight 437.46500
Density 1.38 Boiling Point 678ºC at 760 mmHg
Molecular Formula C22H17F2N5OS Melting Point N/A
MSDS N/A Flash Point 363.8ºC

 Use of Isavuconazole


Isavuconazole is a moderate inhibitor of CYP3A4 and a water-soluble triazole with broad-spectrum antifungal activity.

 Names

Name isavuconazole
Synonym More Synonyms

 Isavuconazole Biological Activity

Description Isavuconazole is a moderate inhibitor of CYP3A4 and a water-soluble triazole with broad-spectrum antifungal activity.
Related Catalog
In Vitro Isavuconazole shows good activity against all Candida spp., with active MIC50 of 0.004 mg/L. The MIC50s/MIC90s range from 0.002/0.004 mg/L for C. albicans to 0.25/0.5 mg/L for C. glabrata[1]. Isavuconazole has potent in vitro activity against most common Aspergillus species, Purpureocillium lilacinum, and Scedosporium apiospermum[2]. Isavuconazole shows potent activity against molds, yeasts, and dimorphic fungi. Rhizopus isolates have MIC values to isavuconazole as low as 0.12 µg/mL with others as high as 32 µg/mL[3]. In the study of pharmacokinetics and pharmacodynamics of isavuconazole against the GFP transformant, F/11628, NIH 4215, and F/16216, the modal MICs of isavuconazole are 1, 8, 1, 4 mg/L, respectively[4].
References

[1]. Seifert H, et al. In vitro activities of isavuconazole and other antifungal agents against Candida bloodstream isolates. Antimicrob Agents Chemother. 2007 May;51(5):1818-21.

[2]. Steinmann J, et al. In Vitro Activity of Isavuconazole against Rasamsonia Species. Antimicrob Agents Chemother. 2016 Oct 21;60(11):6890-6891.

[3]. Donnelley MA, et al. Isavuconazole in the treatment of invasive aspergillosis and mucormycosis infections. Infect Drug Resist. 2016 Jun 2;9:79-86.

[4]. Box H, et al. Pharmacodynamics of Isavuconazole in a Dynamic In Vitro Model of Invasive Pulmonary Aspergillosis. Antimicrob Agents Chemother. 2015 Oct 26;60(1):278-87.

 Chemical & Physical Properties

Density 1.38
Boiling Point 678ºC at 760 mmHg
Molecular Formula C22H17F2N5OS
Molecular Weight 437.46500
Flash Point 363.8ºC
Exact Mass 437.11200
PSA 115.86000
LogP 4.24298

 Precursor & DownStream

Precursor  1

DownStream  0

 Synonyms

4-{2-[(2R,3R)-3-(2,5-difluorophenyl)-3-hydroxy-4-(1H-1,2,4-triazol-1-yl)butan-2-yl]-1,3-thiazol-4-yl}benzonitrile
BAL 4815
UNII-60UTO373KE
4-[2-[(2R,3R)-3-(2,5-difluorophenyl)-3-hydroxy-4-(1,2,4-triazol-1-yl)butan-2-yl]-1,3-thiazol-4-yl]benzonitrile
Isavuconazole
Bal4815
4-{2-[(2R,3R)-3-(2,5-Difluorophenyl)-3-hydroxy-4-(1H-1,2,4-triazol-1-yl)-2-butanyl]-1,3-thiazol-4-yl}benzonitrile
Benzonitrile, 4-[2-[(1R,2R)-2-(2,5-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]-4-thiazolyl]-
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