Mouse and rat pharmacokinetics for abemaciclib using a 30 mg/kg oral dose

Data are mean values from three animals.

Plasma AUC0–24 h (ng·h/ml)69,30052,300
Plasma AUC0–24 h (nM·h)136,686103,156
Unbound plasma AUC0–24 h (nM·h)a73813817
Plasma Tmax (h)b43.3
Plasma Cmax (ng/ml)84701500
Plasma Cmax (nM)16,7062958
Unbound plasma Cmax (nM)a 902109
Brain AUC0–24 h (ng·h/ml)13,20047,900
Brain AUC0–24 h (nM·h)26,03594,447
Unbound brain AUC0–24 h (nM·h)206406
Brain Tmax (h)24
Brain Cmax (ng/ml)18401500
Brain Cmax (nM)36292958
Unbound brain Cmax (nM)a2913
Clearance (ml/min per kg)b4114
Half-life (h)b136
Vd,ss (l/kg)b346.0
Oral bioavailability (%)b6243
  • a Measured fu values from Table 3.

  • b Determined from 1 mg/kg (mouse) or 0.5 mg/kg (rat) i.v. and 3 mg/kg (mouse) or 1.0 mg/kg (rat) p.o. doses.