TABLE 6

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).

CompoundCu,plasmaCu,brainKp,brainKp,uu,brain
NormalKONormalKONormalKONormalKO
nM
Abemaciclib12014120671.23.20.170.48
Palbociclib4783446710.12.30.010.21
  • Kp,brain, brain-to-plasma ratio of the total concentrations; Kp,uu,brain, brain-to-plasma ratio of the unbound concentrations.