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.
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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.
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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.
Regulatory snapshots, including global drug submissions and approvals, clinical trial approvals and other regulatory decisions and designations: Accord, Applied, Astrazeneca, Azitra, Briacell, Glycomine, Imcheck, Merck, Moderna, Nicox, Novartis, Valneva.