Isavuconazonium sulfate

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Chemical Structure| 946075-13-4 同义名 : BAL8557-002;Isavuconazonium (sulfate)
CAS号 : 946075-13-4
货号 : A599121
分子式 : C35H36F2N8O9S2
纯度 : 98%
分子量 : 814.835
MDL号 : MFCD27987905
存储条件:

Pure form Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(128.86 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Isavuconazonium sulfate is a prodrug of isavuconazole, a broad-spectrum mould-active triazole antifungal drug. The MIC values obtained for the prodrug were one 2-fold dilution higher than those of isavuconazole for all isolates tested. The essential agreement (±2 log2 dilutions) between prodrug and isavuconazole MIC values was 96.4% across all tested isolates[3]. Isavuconazonium sulfate, is currently approved in the United States and Europe for the treatment of the two of the most common and most challenging invasive fungal infections in clinical practice, invasive aspergillosis and invasive mucormycosis. It is available in both oral and intravenous formulations for once-a-day dosing and has favorable safety profile and drug interaction potential in comparison to voriconazole[4]. And Isavuconazonium sulfate has demonstrable activity against Candida species and other common fungal pathogens[5]. Similar significant reductions in the fungal burden in the brain and cerebrospinal fluid in rabbits treated with isavuconazonium sulfate and fluconazole compared with that in the untreated controls were observed. Isavuconazonium sulfate, like fluconazole, could be beneficial in the setting of consolidation and maintenance therapy, rather than induction monotherapy, in high-burden cryptococcal meningoencephalitis[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.23mL

0.25mL

0.12mL

6.14mL

1.23mL

0.61mL

12.27mL

2.45mL

1.23mL

参考文献

[1]Townsend R, Kato K, et al. Two Phase 1, Open-Label, Mass Balance Studies to Determine the Pharmacokinetics of (14) C-Labeled Isavuconazonium Sulfate in Healthy Male Volunteers. Clin Pharmacol Drug Dev. 2017 Jul 27.

[2]Traynor K. Isavuconazonium sulfate approved for invasive fungal infections. Am J Health Syst Pharm. 2015 Apr 15;72(8):592.

[3]Pfaller MA, Rhomberg PR, Castanheira M. Direct in vitro comparison of the prodrug isavuconazonium sulfate with the isavuconazole active compound against Aspergillus spp. and 2 rare moulds. Diagn Microbiol Infect Dis. 2018;92(1):43‐45

[4]Walker RC, Zeuli JD, Temesgen Z. Isavuconazonium sulfate for the treatment of fungal infection. Drugs Today (Barc). 2016;52(1):7‐16

[5]Murrell D, Bossaer JB, Carico R, Harirforoosh S, Cluck D. Isavuconazonium sulfate: a triazole prodrug for invasive fungal infections. Int J Pharm Pract. 2017;25(1):18‐30

[6]Kovanda LL, Giamberardino C, McEntee L, et al. Pharmacodynamics of Isavuconazole in a Rabbit Model of Cryptococcal Meningoencephalitis. Antimicrob Agents Chemother. 2019;63(9):e00546-19. Published 2019 Aug 23