Structure-based development and preclinical evaluation of the SARS-CoV-2 3C-like protease inhibitor simnotrelvir

• Published in: Nature communications Vol. 14; no. 1; pp. 6463 - 15
• Main Authors: Jiang, Xiangrui, Su, Haixia, Shang, Weijuan, Zhou, Feng, Zhang, Yan, Zhao, Wenfeng, Zhang, Qiumeng, Xie, Hang, Jiang, Lei, Nie, Tianqing, Yang, Feipu, Xiong, Muya, Huang, Xiaoxing, Li, Minjun, Chen, Ping, Peng, Shaoping, Xiao, Gengfu, Jiang, Hualiang, Tang, Renhong, Zhang, Leike, Shen, Jingshan, Xu, Yechun
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 13.10.2023; Nature Publishing Group; Nature Portfolio
• Subjects: 631/326/22/1295; 631/326/596/4130; 692/308/153; 692/699/255/2514; 82/83; Animals; Antiviral Agents - chemistry; Antiviral Agents - pharmacology; Antiviral Agents - therapeutic use; Bioavailability; Clinical trials; Coronaviruses; COVID-19; Effectiveness; Enthalpy; Enzyme Inhibitors; Female; Humanities and Social Sciences; Humans; Male; Males; Mice; Monkeys; multidisciplinary; Optimization; Pandemics; Pharmacokinetics; Pharmacology; Protease; Protease inhibitors; Protease Inhibitors - chemistry; Protease Inhibitors - pharmacology; Protease Inhibitors - therapeutic use; Proteinase inhibitors; Rats; Ritonavir; Robustness; Safety; SARS-CoV-2; Science; Science (multidisciplinary); Severe acute respiratory syndrome coronavirus 2; Viral diseases

The persistent pandemic of coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and its variants accentuates the great demand for developing effective therapeutic agents. Here, we report the development of an orally bioavailable SARS-CoV-2 3C-lik...