The global pandemic caused by the novel coronavirus, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has had an unprecedented impact on the economy and life of individuals globally, and safe and efficacious oral agents are urgently required. We discovered a non-peptidic, non-covalent SARS-CoV-2 3CL
pro inhibitor S-217622 (Ensitrelvir), which displayed
in vitro and
in vivo antiviral activity with preferable DMPK profile for once-daily oral dosing, using an SBDD strategy. The preclinical data support the suitable pharmaceutical properties of Ensitrelvir as a potential oral therapeutic agent for patients with COVID-19, and in clinical trials started in July 2021, favourable pharmacokinetics (Ph1) and clear antiviral effects (Ph2a and Ph2b) have been confirmed. As of July 2022, Ph3 trials are underway and it has been filed for approval as an Emergency Use Authorization in Japan.
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