TABLE 4

E6201 pharmacokinetic/metric parameters in FVB wild-type mice following administration of single oral dose of 40 mg/kg

Data are presented as mean or mean ± S.E.M. (n = 4).

PlasmaBrain
Half-life (h)1.370.98
Cmax (μg/ml)2.44 ± 0.416.04 ± 1.55
Tmax (h)0.50.5
AUC(0–t) (μg*h/ml)3.94 ± 0.549.23 ± 1.95
AUC(0–∞) (μg*h/ml)4.229.31
CL/F (ml/min per kilogram)158
Vd/F (l/kg)18.7
Kp (AUC(0–t) ratio)-2.35
Kp,uu (AUC(0–t) ratio)-0.13
F0.39
  • AUC(0–t), area under the curve from zero to the time of last measured concentration; AUC(0–∞), area under the curve from zero to time infinity; CL/F, apparent clearance; Cmax, observed maximum concentration; F (absolute bioavailability), ratio of the dose corrected AUC(0–t),PO to dose corrected AUC(0–t),iv; Kp (AUC ratio), the ratio of AUC(0–t,brain) to AUC(0–t,plasma) using total drug concentrations; Kp,uu (AUC ratio), the ratio of AUC(0–t,brain) to AUC(0–t,plasma) using free drug concentrations; PO, by mouth; Tmax, time to reach the maximum concentration; Vd/F, apparent volume of distribution.