MPro Inhibitor 11a

Bofutrelvir (FB2001) is a SARS-CoV-2 main protease Mpro inhibitor with an IC50 value of 53 nM and an EC50 value of 0.53 μM. Bofutrelvir exhibits potent antiviral efficacy against several current SARS-CoV-2 variants with EC50 values of 0.26-0.42 μM. Bofutrelvir has an additive antiviral effect when combined with Remdesivir (HY-104077)[1][2].

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> SARS-CoV

IC50: 53 nM (Mpro)[1]

Bofutrelvir (24 h) shows in vitro activity against SARS-CoV-2 and its variants with EC50 values of 0.42, 0.39, 0.28, 0.27 and 0.26 μM for SARS-CoV-2, SARS-CoV-2 (Alpha), SARS-CoV-2 (Beta), SARS-CoV-2 (Delta) and SARS-CoV-2 (Omicron), respectively[2]. Bofutrelvir inhibits SARS-CoV-2 replication in vero E6 cells in the presence of human serum (1.1-2.4 μM) even at the dose of EC50 values[2]. Bofutrelvir exhibits an additive effect against SARS-CoV-2 in vitro when combined treatment with remdesivi[2].

Bofutrelvir (100 and 200 mg/kg; i.p. once daily on day 0 and twice daily on day 1, 2 and 3 for 4 consecutive days) effectively against SARS-CoV-2 delta variant infection in vivo[2]. Animal Model: K18-hACE2 mice with SARS-CoV-2 delta variant infection[2] Dosage: 100 and 200 mg/kg Administration: Intraperitoneal injection; 100 and 200 mg/kg once daily on day 0 and twice daily on day 1, 2 and 3 for 4 consecutive days Result: Showed a dose-dependent efficacy to virus titers of lung. Effectively reduces the lung viral loads. Dose-dependently showed antiviral activity against the SARS-CoV-2 Delta variant and significantly reduced viral load in mouse lung and brain.

[1]. Ullrich S, Nitsche C. The SARS-CoV-2 main protease as drug target. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127377.  

[2]. Shang W, et al. In vitro and in vivo evaluation of the main protease inhibitor FB2001 against SARS-CoV-2. Antiviral Res. 2022 Dec;208:105450.