Ascletis’ oral drug shows potential for Covid-19 treatment
Ascletis’ oral drug shows potential for Covid-19 treatment

Ascletis’ oral drug shows potential for Covid-19 treatment

Ascletis Pharma has reported that its small-molecule oral drug candidate ASC11 showed potential for the treatment of Covid-19.

Discovered internally using various technologies from the company, including molecular docking, ASC11 is an inhibitor of 3-chymotrypsin-like protease (3CLpro) with worldwide intellectual property rights.

The company plans to submit an Investigational New Drug application for ASC11 in the second half of this year and complete a Phase I clinical trial with healthy participants by the end of the year.

ASC11 showed an antiviral potency (EC₉₀) 31-fold over Nirmatrelvir, 120-fold for S-217622, ​​16-fold and seven-fold over PBI-0451 and EDP-235, respectively, in antiviral cellular assays with infectious SARS-CoV 2.

Furthermore, it was found that the 3CLpro inhibitor retained activity against different variants of SARS-CoV-2 virus.

Molecular docking revealed that ASC11 formed robust hydrogen bonding interaction with 3CLpro’s Glutamic acid 166, made new hydrogen bonds with other vital amino acids of 3CLpro and attached strongly in hydrophobic Pocket 4 of 3CLpro compared to Nirmatrelvir.

This resulted in an increased antiviral potency (EC₉0) of ASC11.

In addition, the safety window of ASC11 (cytotoxicity versus antiviral potency) was over 10,000-fold in Vero E6 cells.

Together with other preclinical findings, such as in vitro metabolism, microsomal stability, Caco-2 permeability and pharmacokinetic studies in animals, ASC11 was found to be a potential antiviral therapy for Covid-19.

Another 3CLpro preclinical candidate from the company also showed antiviral potency and safety window in Vero E6 cells in line with ASC11.

Ascleti’s founder, chairman and CEO Dr Jinzi Wu said: “We are excited about our small molecule oral preclinical drug candidates for their potential to be the best antiviral treatment of Covid-19.

“These preclinical drug candidates demonstrate our ability to detect as a leading antiviral biotechnology.”

This January, the company dosed the first subject in the phase III study with ASC40 plus bevacizumab for the treatment of recurrent glioblastoma.

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