Summary of pharmacodynamic parameter estimates for H3K27me3 inhibition and antitumor efficacy by PF06821497 in DLBCL xenograft models
The unbound concentrations (EC50, EC70, and Tsc) were calculated from the total concentrations after the correction for an unbound fraction in mouse plasma (0.21).
| In vivo response | Model | EC50 | EC70 | Tsc |
|---|---|---|---|---|
| nM free | nM free | nM free | ||
| H3K27me3 inhibition | I | 76 | 177 | − |
| Tumor growth inhibition | IV | − | − | 161 |
−, not applicable.