Bofutrelvir (FB2001) is a potent, selective and covalent SARS-CoV-2 main protease (Mpro) inhibitor with IC50 value of 53 nM.
Bofutrelvir (FB2001) covalently binds to cysteine 145 of Mpro.
Bofutrelvir (FB2001) shows antiviral activity against several current SARS-CoV-2 variants in vitro.
Bofutrelvir (FB2001) potently inhibitsthe replication of SARS-CoV-2 variants (B.1.1.7 (Alpha): EC50=0.39 μM, B.1.351 (Beta): EC50=0.28 μM; B.1.617.2 (Delta): EC50=0.27 μM; B.1.1.529 (Omicron): EC50=0.26 μM) in Vero E6 cells.
Combined treatment with remdesivir and FB2001 exhibits an additive effect against SARS-CoV-2 in vitro.
Bofutrelvir (FB2001) (100 mpk) exhibits in vivo inhibitory activity of FB2001 in K18-hACE2 mice model of SARS-CoV-2 delta variant infection.
