Nirmatrelvir CAS# 2628280-40-8 帕罗韦德

Nirmatrelvir (PF-07321332) is a potent, selective, orally active inhibitor of the SARS-CoV-2 3CL protease (Mpro). In preclinical enzymatic assays, it inhibited Mpro with a Ki of ~3 nM and showed high selectivity over human proteases. In cell-based antiviral assays, nirmatrelvir suppressed SARS-CoV-2 replication with EC50 values of ~0.04–0.1 µM across multiple variants. In mouse models of SARS-CoV-2 infection, oral dosing significantly reduced viral lung titers and improved pulmonary pathology, particularly when combined with ritonavir to enhance exposure. Pharmacokinetic studies demonstrated good oral bioavailability, high lung penetration, and sustained target engagement, supporting its advancement as an oral antiviral therapy.