Leritrelvir (RAY1216) is a potent, selective peptidomimetic inhibitor of SARS-CoV-2 main protease (Mpro) with Ki of 8.4 nM.
RAY1216 displays high potency against different SARS-CoV-2 variants with EC50 of 116 nM (wild type (WT)), 80 nM (Alpha), 88 nM (Beta), 69 nM (Delta), 81 nM (Omicron BA.1), 91 nM (Omicron BA.5) and 135 nM (Omicron XBB.1.9.1).
RAY1216 (150-600 mg/kg) effectively prolonged survival of mice infected with SARS-CoV-2, significantly decreased lung viral titres.
RAY1216 possesses superior drug-target residence time, when compared with PF-07321332 (nirmatrelvir), the active antiviral component in Paxlovid.
