2. Academic Validation
  3. An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19

An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19

  • Science. 2021 Dec 24;374(6575):1586-1593. doi: 10.1126/science.abl4784.
Dafydd R Owen 1,  Charlotte M N Allerton 1,  Annaliesa S Anderson 2,  Lisa Aschenbrenner 3,  Melissa Avery 3,  Simon Berritt 3,  Britton Boras 4,  Rhonda D Cardin 2,  Anthony Carlo 3,  Karen J Coffman 3,  Alyssa Dantonio 3,  Li Di 3,  Heather Eng 3,  RoseAnn Ferre 4,  Ketan S Gajiwala 4,  Scott A Gibson 5,  Samantha E Greasley 4,  Brett L Hurst 5,  Eugene P Kadar 3,  Amit S Kalgutkar 1,  Jack C Lee 3,  Jisun Lee 3,  Wei Liu 4,  Stephen W Mason 2,  Stephen Noell 3,  Jonathan J Novak 3,  R Scott Obach 3,  Kevin Ogilvie 3,  Nandini C Patel 1,  Martin Pettersson 1,  Devendra K Rai 2,  Matthew R Reese 3,  Matthew F Sammons 1,  Jean G Sathish 2,  Ravi Shankar P Singh 1,  Claire M Steppan 3,  Al E Stewart 4,  Jamison B Tuttle 1,  Lawrence Updyke 1,  Patrick R Verhoest 1,  Liuqing Wei 3,  Qingyi Yang 1,  Yuao Zhu 2
Affiliations

Affiliations

  • 1 Pfizer Worldwide Research, Development & Medical, Cambridge, MA 02139, USA.
  • 2 Pfizer Worldwide Research, Development & Medical, Pearl River, NY 10965, USA.
  • 3 Pfizer Worldwide Research, Development & Medical; Groton, CT 06340, USA.
  • 4 Pfizer Worldwide Research, Development & Medical, La Jolla, CA 92121, USA.
  • 5 Institute for Antiviral Research, Department of Animal, Dairy, and Veterinary Sciences, Utah State University; Logan, UT 84322, USA.
PMID: 34726479 DOI: 10.1126/science.abl4784
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.

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