Fosravuconazole L-lysine ethanolate
Fosravuconazole L-lysine ethanolate Basic information
- Product Name:
- Fosravuconazole L-lysine ethanolate
- Synonyms:
-
- L-Lysine, coMpd. with 4-[2-[(1R,2R)-2-(2,4-difluorophenyl)-1-Methyl-2-[(phosphonooxy)Methoxy]-3-(1H-1,2,4-triazol-1-yl)propyl]-4-thiazolyl]benzonitrile and ethanol (1:1:1) (9CI)
- Fosravuconazole L-lysine ethanolate
- BMS-379224 L-lysine ethanolate
- E-1224 L-lysine ethanolate
- Fungal,onychomycosis,Fosravuconazole Llysine ethanolate,Parasite,parasitemia,inhibit,Fosravuconazole L lysine ethanolate,antifungal,Ravuconazole,Inhibitor,candidiasis,Fosravuconazole L-lysine
- (S)-2,6-Diaminohexanoic acid (((2R,3R)-3-(4-(4-cyanophenyl)thiazol-2-yl)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)butan-2-yl)oxy)methyl dihydrogen phosphate and ethanol salt
- CAS:
- 914361-45-8
- MF:
- C31H40F2N7O8PS
- MW:
- 739.73
- Product Categories:
-
- API
- Mol File:
- 914361-45-8.mol
Fosravuconazole L-lysine ethanolate Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO : 50 mg/mL (67.59 mM; Need ultrasonic)| (insoluble)
- form
- Solid
- color
- White to yellow
- Water Solubility
- Water : < 0.1 mg/mL (ultrasonic)
Fosravuconazole L-lysine ethanolate Usage And Synthesis
Uses
Fosravuconazole L-lysine ethanolate (BMS-379224 L-lysine ethanolate), a proagent of Ravuconazole, is an orally active broad spectrum antifungal agent. Fosravuconazole L-lysine ethanolate can be used for candidiasis, onychomycosis and parasitemia research[1][2][3].
Biological Activity
Fosravuconazole L-lysine ethanolate (BMS-379224 L-lysine ethanolate), a prodrug of Ravuconazole, is an orally active broad-spectrum antifungal agent. Fosravuconazole L-lysine ethanolate can be used in the study of candidiasis, onychomycosis and parasitic diseases.
in vitro
Fosravuconazole has potent in vitro antifungal activity against a wide range of fungal species, including Candida , Aspergillus , and Trichophyton species .
in vivo
Fosravuconazole (E-1224; 10-50 mg/kg; oral administration; daily; for 20 days) treatment suppresses the parasitemia and prevents death in mice infected with the T. cruzi Y strain.
| Animal Model: | Swiss female mice (20-24 g) inoculated with trypomastigotes (Y strain). |
| Dosage: | 10 mg/kg, 20 mg/kg, 30 mg/kg, 40 mg/kg , 50 mg/kg |
| Administration: | Oral administration; daily; for 20 days |
| Result: | Suppressed the parasitemia and prevented death. |
References
[1] Shinichi Watanabe, et al. Efficacy and safety of fosravuconazole L-lysine ethanolate, a novel oral triazole antifungal agent, for the treatment of onychomycosis: A multicenter, double-blind, randomized phase III study. J Dermatol. 2018 Oct;45(10):1151-1159. DOI:10.1111/1346-8138.14607
[2] Katsura Hata, et al. Development of E1224 by leveraging a strategic partnership for the medicines creation against neglected tropical diseases. Parasitol Int. 2020 Dec 25;81:102278. DOI:10.1016/j.parint.2020.102278
[3] Lívia de Figueiredo Diniz, et al. Outcome of E1224-Benznidazole Combination Treatment for Infection with a Multidrug-Resistant Trypanosoma cruzi Strain in Mice. Antimicrob Agents Chemother. 2018 May 25;62(6):e00401-18. DOI:10.1128/AAC.00401-18
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