COVID-19, caused by SARS-CoV-2, is a global pandemic. 3CL protease, essential for coronavirus replication, lacks close human analogs. PF-00835231, a 3CL protease inhibitor, shows potent in vitro antiviral activity. This paper details PF-07304814, a phosphate prodrug of PF-00835231, designed for improved delivery and sustained systemic exposure. PF-00835231 exhibits broad-spectrum activity against coronaviruses and additive/synergistic effects with remdesivir. ADME, safety, in vitro, and in vivo data support clinical evaluation of PF-07304814 as a potential COVID-19 treatment.
Publisher
Nature Communications
Published On
Oct 18, 2021
Authors
Britton Boras, Rhys M. Jones, Brandon J. Anson, Dan Arenson, Lisa Aschenbrenner, Malina A. Bakowski, Nathan Beutler, Joseph Binder, Emily Chen, Heather Eng, Holly Hammond, Jennifer Hammond, Robert E. Haupt, Robert Hoffman, Eugene P. Kadar, Rob Kania, Emi Kimoto, Melanie G. Kirkpatrick, Lorraine Lanyon, Emma K. Lendy, Jonathan R. Lillis, James Logue, Suman A. Luthra, Chunlong Ma, Stephen W. Mason, Marisa E. McGrath, Dafydd Owen, R. Scott Obach, Matthew N. O'Brien, Rebecca O'Connor, Kevin Ogilvie, Martin Pettersson, Matthew R. Reese, Thomas F. Rogers, Romel Rosales, Michelle I. Rossulek, Jean G. Sathish, Norimitsu Shirai, Claire Steppan, Martyn Ticehurst, Lawrence W. Updyke, Stuart Weston, Yuao Zhu, Kris M. White, Adolfo García-Sastre, Jun Wang, Arnab K. Chatterjee, Andrew D. Mesecar, Matthew B. Frieman, Annaliesa S. Anderson, Charlotte Allerton
Tags
COVID-19
SARS-CoV-2
3CL protease inhibitor
PF-07304814
antiviral activity
clinical evaluation
therapeutic options
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