Discovery of a Novel Inhibitor of Coronavirus 3CL Protease for the Potential Treatment of COVID-19

  1. Britton Boras
  2. Rhys M. Jones
  3. Brandon J. Anson
  4. Dan Arenson
  5. Lisa Aschenbrenner
  6. Malina A. Bakowski
  7. Nathan Beutler
  8. Joseph Binder
  9. Emily Chen
  10. Heather Eng
  11. Holly Hammond
  12. Jennifer Hammond
  13. Robert E. Haupt
  14. Robert Hoffman
  15. Eugene P. Kadar
  16. Rob Kania
  17. Emi Kimoto
  18. Melanie G. Kirkpatrick
  19. Lorraine Lanyon
  20. Emma K. Lendy
  21. Jonathan R. Lillis
  22. James Logue
  23. Suman A. Luthra
  24. Chunlong Ma
  25. Stephen W. Mason
  26. Marisa E. McGrath
  27. Stephen Noell
  28. R. Scott Obach
  29. Matthew N. O’Brien
  30. Rebecca O’Connor
  31. Kevin Ogilvie
  32. Dafydd Owen
  33. Martin Pettersson
  34. Matthew R Reese
  35. Thomas F. Rogers
  36. Michelle I. Rossulek
  37. Jean G. Sathish
  38. Norimitsu Shirai
  39. Claire Steppan
  40. Martyn Ticehurst
  41. Lawrence W. Updyke
  42. Stuart Weston
  43. Yuao Zhu
  44. Jun Wang
  45. Arnab K. Chatterjee
  46. Andrew D. Mesecar
  47. Matthew B. Frieman
  48. Annaliesa S. Anderson
  49. Charlotte Allerton
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Abstract

COVID-19 caused by the SARS-CoV-2 virus has become a global pandemic. 3CL protease is a virally encoded protein that is essential across a broad spectrum of coronaviruses with no close human analogs. The designed phosphate prodrug PF-07304814 is metabolized to PF-00835321 which is a potent inhibitorin vitroof the coronavirus family 3CL pro, with selectivity over human host protease targets. Furthermore, PF-00835231 exhibits potentin vitroantiviral activity against SARS-CoV-2 as a single agent and it is additive/synergistic in combination with remdesivir. We present the ADME, safety,in vitro, andin vivoantiviral activity data that supports the clinical evaluation of this compound as a potential COVID-19 treatment.

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