In vitro and in vivo evaluation of the main protease inhibitor FB2001 against SARS-CoV-2.

ABSTRACT: FB2001 is a drug candidate that targets the main protease of SARS-CoV-2 via covalently binding to cysteine 145. In this study, we evaluated the inhibitory activities of FB2001 against several SARS-CoV-2 variants in vitro and in vivo (in mice), and we also evaluated the histopathological analysis and immunostaining of FB2001 on lung and brain which have been rarely reported. The results showed that FB2001 exhibited potent antiviral efficacy against several current SARS-CoV-2 variants in Vero E6 cells, namely, B.1.1.7 (Alpha): EC₅₀ = 0.39 ± 0.01 μM, EC₉₀ = 0.75 ± 0.01 μM; B.1.351 (Beta): EC₅₀ = 0.28 ± 0.11 μM, EC₉₀ = 0.57 ± 0.21 μM; B.1.617.2 (Delta): EC₅₀ = 0.27 ± 0.05 μM, EC₉₀ = 0.81 ± 0.20 μM; B.1.1.529 (Omicron): EC₅₀

SUBMITTER: Shang W 

PROVIDER: S-EPMC9617675 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature