Therapy Areas: Infectious Diseases
Ascletis reveals the 3CLpro inhibitor ASC11 is effective against COVID-19
19 April 2022 -

R&D biotech company Ascletis Pharma Inc (HKEX:1672) on Tuesday said its oral small molecule drug candidate ASC11 shows to be an effective treatment for COVID-19 as well as the ASC11 activity was retained against different SARS-CoV-2 variants.

ASC11, which is a 3-chymotrypsin like protease (3CLpro) inhibitor, is an in-house discovered oral small molecule drug candidate using various proprietary technologies including molecular docking. ASC11 has global intellectual property rights, added the company.

Based on antiviral cellular assays with infectious SARS-CoV-2, the antiviral potency (EC90) of ASC11 is 31-fold of that of Nirmatrelvir, 120-fold (600/5) of that of S-217622, 16-fold of that of PBI-0451 as well as seven fold of that of EDP-235.

In Vero E6 cells, the safety window of ASC11 is more than 10,000-fold. Based on other preclinical data including Caco-2 permeability, in vitro metabolism, microsomal stability and animal pharmacokinetic studies, ASC11 demonstrated potential for best-in-class antiviral treatment of COVID-19.

According to the company, it plans to file its Investigational New Drug (IND) of ASC11 in the second half of 2022 and complete Phase I clinical trial in healthy subjects by the end of 2022. The second 3CLpro preclinical candidate (PCC), which is discovered in-house with global intellectual property rights, demonstrated the same antiviral potency and safety window in Vero E6 cells as compared to ASC11.

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