| Literature DB >> 34726479 |
Dafydd R Owen1, Charlotte M N Allerton1, Annaliesa S Anderson2, Lisa Aschenbrenner3, Melissa Avery3, Simon Berritt3, Britton Boras4, Rhonda D Cardin2, Anthony Carlo3, Karen J Coffman3, Alyssa Dantonio3, Li Di3, Heather Eng3, RoseAnn Ferre4, Ketan S Gajiwala4, Scott A Gibson5, Samantha E Greasley4, Brett L Hurst5, Eugene P Kadar3, Amit S Kalgutkar1, Jack C Lee3, Jisun Lee3, Wei Liu4, Stephen W Mason2, Stephen Noell3, Jonathan J Novak3, R Scott Obach3, Kevin Ogilvie3, Nandini C Patel1, Martin Pettersson1, Devendra K Rai2, Matthew R Reese3, Matthew F Sammons1, Jean G Sathish2, Ravi Shankar P Singh1, Claire M Steppan3, Al E Stewart4, Jamison B Tuttle1, Lawrence Updyke1, Patrick R Verhoest1, Liuqing Wei3, Qingyi Yang1, Yuao Zhu2.
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.Entities:
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Year: 2021 PMID： 34726479 DOI： 10.1126/science.abl4784
Source DB: PubMed Journal: Science ISSN： 0036-8075 Impact factor: 47.728