开发超纯和强大的酸作为泛冠状病毒抗病毒治疗药物
Po-Chang Shih1, Yi-Wen Mao1, Jhe-Wei Hu1
1Department of Research and Development, SyneuRx International (Taiwan) Corp., New Taipei City 22175, Taiwan.
ACS pharmacology & translational science
|August 15, 2023
概括
潘塔兰迪尔的超纯和强阳酸 (UPPTA) 通过抑制病毒复制,对SARS-CoV-2和HCoV-OC43表现出广泛的抗病毒活性. 这种有前途的泛冠病毒候选药物显示出安全的毒理学特征,并正在推进临床试验.
科学领域:
- 病毒学 病毒学
- 药物发现 药物发现 药物发现
- 生物化学 生物化学
背景情况:
- 冠状病毒的持续威胁需要开发广泛的抗病毒药物.
- 不同的冠状病毒菌株,包括SARS-CoV-2和HCoV-OC43,对公共卫生构成重大挑战.
研究的目的:
- 评估Pentarlandir超纯强酸 (UPPTA) 对SARS-CoV-2和HCoV-OC43的抗病毒疗效和安全性.
- 调查UPPTA的作用机制和药理动力学特性.
主要方法:
- 生物化学分析和3 - 胆素样蛋白酶 (3CLpro) 试验被使用.
- 使用基于细胞的病毒杀伤性,细胞毒性和功能增益测试.
- 进行了药理动力学和毒理学研究.
主要成果:
- UPPTA对SARS-CoV-2 (EC50 ≈ 0.5 μM) 和HCoV-OC43 (EC50 ≈ 1.3 μM) 均表现出强大的抗病毒活性.
- 药物的机制包括抑制3CLpro酶,这对病毒复制至关重要.
- UPPTA显示出有利的药理动力学,具有高肺分布和出色的安全性.
结论:
- UPPTA被确定为安全有效的泛冠病毒抗病毒药物候选者.
- 该化合物的抑制3CLpro的能力及其有利的安全性概况支持其进入临床开发.
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