Tecovirimat monohydrate  (Synonyms: ST-246 monohydrate)

Tecovirimat (ST-246) monohydrate is the monohydrate form of Tecovirimat (HY-14805). Tecovirimat monohydrate is an orally bioavailable and selective compound against orthopoxviruses [including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), smallpox and variola viruses]. Tecovirimat monohydrate is evaluated against vaccinia, cowpox virus, ectromelia virus with EC₅₀ values of 0.01 μM, 0.48 μM and 0.05 μM, respectively. Tecovirimat monohydrate targets the orthopoxvirus protein VP37 which is necessary for membrane envelopment of intracellular mature virus particles to form enveloped virus. Tecovirimat monohydrate exerts antiviral activity on the target of the cowpox virus V061 gene, which is homologous to vaccinia virus F13L, encoding a major envelope protein (p37) required for production of extracellular virus. Tecovirimat monohydrate could be used in the study for orthopoxvirus-induced diseases^{[1][2][3][4][5]}.

Tecovirimat monohydrate (0-50 μM，3 天) 是一种有效的特异性正痘病毒复制抑制剂，对广泛的正痘病毒都有效^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Tecovirimat monohydrate (50 mg/kg，口服强饲法，一天两次，持续 14 天) 在致死性鼻内牛痘病毒小鼠模型中给药对牛痘病毒感染产生保护性免疫反应^[1]。
Tecovirimat monohydrate (50 mg/kg，口服强饲法，5 天) 在牛痘病毒-小鼠尾部病变模型中能抑制牛痘病毒诱导的病变形成^[1]。
Tecovirimat monohydrate (100 mg/kg，口服，每天一次，间断 5，7，10 或 14 天) 显著降低了牛痘病毒 (CV) 感染小鼠的死亡率^[2]。

ST-246在小鼠体内的药动学参数^[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

394.34

C₁₉H₁₇F₃N₂O₄

1162664-19-8

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Quenelle DC, et al. Efficacy of delayed treatment with ST-246 given orally against systemic orthopoxvirus infections in mice[J]. Antimicrob Agents Chemother. 2007 Feb;51(2):689-95.  [Content Brief]

  [2]. DeLaurentis CE, et al. New Perspectives on Antimicrobial Agents: Tecovirimat monohydrate for Treatment of Human Monkeypox Virus[J]. Antimicrob Agents Chemother. 2022 Dec 20;66(12):e0122622.  [Content Brief]

  [3]. Yang G, et al. An orally bioavailable antipoxvirus compound (ST-246) inhibits extracellular virus formation and protects mice from lethal orthopoxvirus Challenge[J]. J Virol. 2005 Oct;79(20):13139-49.  [Content Brief]

  [4]. Russo AT, et al. An overview of Tecovirimat monohydrate for smallpox treatment and expanded anti-orthopoxvirus applications[J]. Expert Rev Anti Infect Ther. 2021 Mar;19(3):331-344.  [Content Brief]

  [5]. TYAVANAGIMATT SR, et al., Rehydration of micronized tecovirimat monohydrate. WO2015077143.

  [6]. Almehmadi M, et al. A Glance at the Development and Patent Literature of Tecovirimat monohydrate: The First-in-Class Therapy for Emerging Monkeypox Outbreak[J]. Viruses. 2022 Aug 25;14(9):1870.  [Content Brief]