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. 2021 Oct 18;12:6055. doi: 10.1038/s41467-021-26239-2

Fig. 6. PF-07304814 (prodrug) and PF-00835231 in vivo exposure summary.

Fig. 6

A Rat, dog and monkey PK following IV administration of PF-07304814 (1.17 mg/kg) or PF-00835231 (2 mg/kg rat, 1 mg/kg dog and monkey) demonstrating high levels of PF-00835231 formed in vivo. (n = 2 or 3; individual data points plotted). B Predicted human PK parameters and measured protein binding for PF-07304814 and PF-00835231 used for human dose prediction. C Projected human systemic exposure profiles at the minimally efficacious dose of 500 mg/day of PF-07304814 delivered as a continuous IV infusion. The predicted unbound steady-state concentrations for the prodrug PF-07304814 (purple) and the active moiety PF-00835231 (blue) are 0.17 µM and 0.5 µM respectively. (NOAEL = No Observed Adverse Effect Level; Ceff = projected minimally efficacious concentration, Fu= unbound fraction; Clp= Plasma Clearance; Vdss= Volume of distribution steady state, Cssu = unbound steady-state concentration).