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ALG-097558的发现和临床前资料,一种泛冠状病毒3CLpro抑制剂

Dorothée Bardiot¹, David C McGowan², Kusum Gupta³

¹CISTIM Leuven vzw, Gaston Geenslaan 2, 3001 Leuven, Belgium.

Journal of medicinal chemistry

|June 30, 2025

概括

一种针对SARS-CoV-2主要蛋白酶的新口服药物显示出治疗冠状病毒的前景. 这种可逆的共价抑制剂在子中显示出有效性,并且可能允许每天服用两次,而无需增强剂.

科学领域:

病毒学和药物发现
药用化学医学化学

背景情况:

2019年SARS-CoV-2流行病造成了全球健康和经济的重大破坏.
SARS-CoV-2 主蛋白酶 (3CLpro) 对于病毒复制至关重要,使其成为关键的治疗点.

研究的目的:

发现和描述一种新的,口服可用的SARS-CoV-2主要蛋白酶的抑制剂.
评估该化合物对SARS-CoV-2和其他人类冠状病毒的疗效.
评估人类简化剂量方案的潜力.

主要方法:

发现一种可逆的共价抑制剂,ALG-097558 (化合物7).
在叙利亚仓鼠感染模型中进行了体外和体内疗效研究.
在临床前物种中进行药理动力学 (PK) 研究,以预测人类PK.
评估对药物动力学增强剂的需求.

主要成果:

ALG-097558是一种口服可用的,可逆的共价抑制剂,用于SARS-CoV-2 3CLpro.
该化合物对多种人类冠状病毒表现出高活性.
在低度的血模型中观察到口服疗效.
预计的人类PK表明潜在的每日两次 (BID) 剂量没有里托纳维尔.

结论:

ALG-097558代表了治疗SARS-CoV-2和潜在的其他冠状病毒感染的有希望的治疗候选者.
药物的概况表明了简化剂量方案,可能会改善患者的服药性.
在临床前评估后,ALG-097558已进入1期临床试验.

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