An Oral SARS-CoV-2 M pro Inhibitor Clinical Candidate for the Treatment of COVID-19

  1. Dafydd R Owen
  2. Charlotte M N Allerton
  3. Annaliesa S Anderson
  4. Lisa Aschenbrenner
  5. Melissa Avery
  6. Simon Berritt
  7. Britton Boras
  8. Rhonda D Cardin
  9. Anthony Carlo
  10. Karen Coffman
  11. Alyssa Dantonio
  12. Li Di
  13. Heather Eng
  14. RoseAnn Ferre
  15. Ketan S Gajiwala
  16. Scott A Gibson
  17. Samantha E Greasley
  18. Brett L Hurst
  19. Eugene P Kadar
  20. Amit S Kalgutkar
  21. Jack C Lee
  22. Jisun Lee
  23. Wei Liu
  24. Stephen W Mason
  25. Stephen Noell
  26. Jonathan J Novak
  27. R Scott Obach
  28. Kevin Ogilvie
  29. Nandini C Patel
  30. Martin Pettersson
  31. Devendra K Rai
  32. Matthew R Reese
  33. Matthew F Sammons
  34. Jean G Sathish
  35. Ravi Shankar P Singh
  36. Claire M Steppan
  37. Al E Stewart
  38. Jamison B Tuttle
  39. Lawrence Updyke
  40. Patrick R Verhoest
  41. Liuqing Wei
  42. Qingyi Yang
  43. Yuao Zhu
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Abstract

The worldwide outbreak of coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has become an established global pandemic. Alongside vaccines, antiviral therapeutics are an important part of the healthcare response to counter 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 I clinical trial in healthy human participants. Clinical Trial Registration ID #: <ext-link xmlns:xlink="http://www.w3.org/1999/xlink" ext-link-type="clintrialgov" xlink:href="NCT04756531">NCT04756531</ext-link>

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