PF-07304814 is a phosphate prodrug of PF-00835231 that binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174?nM.
Lufotrelvir (PF-07304814) is a phosphate prodrug of PF-00835231, and there is no statistical difference in antiviral potency of Lufotrelvir in vero cells expressing high levels of the efflux transporter P-glycoprotein, showing strong antiviral activity by inhibiting coronavirus family 3CL protease activity.[1]
PF-07304814 exhibits high conversion to PF-00835231, systemic clearance and short half-life across species in rats, dogs, and monkey, respectively, also shows unbound CLint values of 51, 84, 168 and 428??L/min/mg in rat, dog, monkey and human respectively. [1]
[1] Britton Boras, et al. Nat Commun . 2021 Oct 18;12(1):6055.