MBUA results for abemaciclib and palbociclib in CF-1 (normal) or CF-1 mdr1a(−/−) mice
Total concentrations in plasma and brain were measured 5 minutes after an intravenous dose of 2.2 µmol/kg. Brain concentrations were corrected for plasma volume, and unbound concentrations were calculated using the measured unbound fraction (Table 4).
| Compound | Cu,plasma | Cu,brain | Kp,brain | Kp,uu,brain | ||||
|---|---|---|---|---|---|---|---|---|
| Normal | KO | Normal | KO | Normal | KO | Normal | KO | |
| nM | ||||||||
| Abemaciclib | 120 | 141 | 20 | 67 | 1.2 | 3.2 | 0.17 | 0.48 |
| Palbociclib | 478 | 344 | 6 | 71 | 0.1 | 2.3 | 0.01 | 0.21 |
Kp,brain, brain-to-plasma ratio of the total concentrations; Kp,uu,brain, brain-to-plasma ratio of the unbound concentrations.