In work at Shanghai Curegene Pharmaceutical Co. Ltd., synthesis and optimization of a series of SARS-CoV-2 3CL protease (3CLpro, Mpro) inhibitors led to the identification of compounds [I], [II] and [III] as lead candidates suitable for further evaluation, based on their enzymatic IC50s (14, 12 and 8.6 nM, respectively), cellular EC50s (36, 26 and 52 nM, respectively) and human liver microsome (HLM) stability.
Details on the work leading to the discovery of the second-generation SARS-CoV-2 main protease (Mpro) inhibitor PF-7817883 (ibuzatrelvir) were disclosed recently by Pfizer Inc. The drug is in phase II clinical development for the treatment of adult individuals with COVID-19 symptoms who are not hospitalized.
Insilico Medicine Inc. has synthesized 3C-like proteinase (3CLpro; Mpro; nsp5) (SARS-CoV-2; COVID-19 virus) inhibitors reported to be useful for the treatment of SARS-CoV-2 infection (COVID-19).
The State University of New Jersey (Rutgers) has synthesized non-structural protein 3 (nsp3; PL-pro) (SARS-CoV-2; COVID-19 virus) inhibitors reported to be useful for the treatment of viral infections.
Ascletis Bioscience Co. Ltd. has patented nucleoside and nucleotide analogues reported to be useful for the treatment of SARS-CoV-2 infection (COVID-19).
Rockefeller University has disclosed non-structural protein 3 (nsp3; PL-PRO) (SARS-CoV-2; COVID-19 virus) inhibitors reported to be useful for the treatment of SARS-CoV-2 infection (COVID-19).
Researchers have identified a gene associated with whether patients hospitalized with respiratory viral infections recover rapidly or face life-threatening complications. The gene has the potential to be used as a diagnostic tool or biomarker, which could help triage patients suffering from severe respiratory infections. Having such a biomarker would help clinicians in their early risk assessments to manage their intervention strategies.
Merck Sharp & Dohme LLC has disclosed 3C-like proteinase (3CLpro; Mpro; nsp5) (SARS-CoV-2; COVID-19 virus) inhibitors reported to be useful for the treatment of SARS-CoV-2 infection (COVID-19).
Armed with $55 million in series A funds and a U.S. government contract, Cambridge, Mass.-based Red Queen Therapeutics Inc. launched operations this week, with plans to advance its novel stapled lipopeptide platform, which creates new antiviral therapies that do not rely on the immune system to work.
