A new Science study details PF-07321332, an orally active, small-molecule inhibitor of the SARSCoV2 main protease, a key viral target. In a phase I clinical trial, it achieved concentrations expected to inhibit the virus based on in vitro studies. pfizer
=90.5 ng/ml, 181 nM) at 12 hours after dose, thus increasing confidence in achieving robust pan-coronavirus antiviral activity clinically . On the basis of these observations and the high safety margins at the NOAEL doses in animals, the efficacy of PF-07321332 in COVID-19 patients will be assessed with a twice-daily dosing paradigm with the potential to increase the dose of PF-07321332 as a single agent and/or co-administered with RTV.
This research used resources of the Advanced Photon Source, a US Department of Energy Office of Science User Facility operated for the DOE Office of Science by Argonne National Laboratory under contract no. DE-AC02-06CH11357. Extraordinary facility operations were supported in part by the DOE Office of Science through the National Virtual Biotechnology Laboratory, a consortium of DOE national laboratories focused on the response to COVID-19, with funding provided by the Coronavirus CARES Act.
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