Prediction of in vivo CL in mouse from in vitro data for four ALK inhibitor analogs
| Compound | CLint,max | fu,mic | fub | Predicted CL | In Vivo CL | Observed/Predicted | |||
|---|---|---|---|---|---|---|---|---|---|
| Plasma | Liver Microsomes | Plasma | Hepatic | ||||||
| Hydrolysis | Hydrolysis | NADPH-Dependent | |||||||
| μl/min⋅ml | μl/min⋅mg | l/h⋅kg | |||||||
| 1 | 71.4 | 1876 | 173 | 0.76 | 0.020 | 0.21 | 3.8 | 5.52 | 1.4 |
| 2 | 10.7 | 175 | 153 | 0.53 | 0.046 | 0.031 | 3.0 | 3.51 | 1.2 |
| 3 | 2.09 | 47.0 | 147 | 0.22 | 0.011 | 0.0061 | 1.6 | 2.14 | 1.3 |
| 4 | 1.68 | 20.6 | 99.5 | 0.22 | 0.012 | 0.0049 | 1.2 | 2.66 | 2.2 |