Sunshine Biopharma Inc. announced it has developed an orally active protease inhibitor that showed dose-dependent antiviral activity in mice infected with SARS-CoV-2.
The Agency for Science Technology & Research (A*STAR) Bioprocessing Technology Institute has patented 3C-like proteinase (3CLpro; Mpro; nsp5) (coronavirus) inhibitors.
Westlake Pharmaceutical (Hangzhou) Co. Ltd. has prepared and tested new 3C-like proteinase (3CLpro; Mpro; nsp5) inhibitors reported to be useful for the treatment of coronavirus acute respiratory syndrome.
One of the challenges associated with COVID-19 has been an increase of secondary infections, including fungal infections. These coinfections can hinder treatment efficacy and increase illness severity.
The COVID-19 pandemic pushed the urgency for effective antiviral drugs against coronaviruses. Researchers from Europe conducted machine learning and in vitro validation experiments for the identification of potential antiviral drugs effective against coronaviruses.
Tohoku University has disclosed 3C-like proteinase (3CLpro; Mpro; nsp5) (SARS-CoV-2; COVID-19 virus) inhibitors reported to be useful for the treatment of viral infections and inflammatory disorders.
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.
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