Abstract
The worldwide outbreak of COVID-19 caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has become a global pandemic. Alongside vaccines, antiviral therapeutics are an important part of the healthcare response to countering the ongoing threat presented by COVID-19. Here, we report the discovery and characterization of PF-07321332, an orally bioavailable SARS-CoV-2 main protease inhibitor with in vitro pan-human coronavirus antiviral activity and excellent off-target selectivity and in vivo safety profiles. PF-07321332 has demonstrated oral activity in a mouse-adapted SARS-CoV-2 model and has achieved oral plasma concentrations exceeding the in vitro antiviral cell potency in a phase 1 clinical trial in healthy human participants.
Highlights
First release: 2 November 2021 www.sciencemag.org (Page numbers not final at time of first release) 1 μ μ μ α www.sciencemag.org (Page numbers not final at time of first release) 2 μ μ μ www.sciencemag.org (Page numbers not final at time of first release) 3 μ μ μ www.sciencemag.org (Page numbers not final at time of first release) 4 α α.
Summary
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