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Estimated PD parameters of dasatinib and ponatinib in orally-dosed mice
| Dasatinib | Ponatinib | |
|---|---|---|
| Emax (ng/ml) (CV%) | 7.3 (67%) | 2.6 (56%) |
| EC50 (ng/ml) (CV%) | 32.0 (69%) | 50.2 (47%) |
| EC90 (ng/ml) (CV%) | 33.0 (14%) | 63.0 (13%) |
| Maximum pLCK inhibition (%) (CV%) | 88.0 (8%) | 72.0 (16%) |
| Median duration of pLCK/LCK <50% (hrs/day) (10th-90th percentile) | 20 mg/kg 10.0 (4.7, 19.7) | 15 mg/kg 10.5 (0, 24.0) |
| 40 mg/kg 15.5 (8.9, 24.0) | 30 mg/kg 14.8 (0, 24.0) |
PD, pharmacodynamic.
