TABLE 2

Pharmacokinetic parameters in wild-type mice

The values were larger than the half-life in plasma because the complete elimination phase was not captured in the experiments.

UnitAEE788AfatinibAZD3759DacomitinibErlotinibGefitinibOsimertinibVandetanib
thalfh12.47.202.378.450.8272.662.7713.7
Apparent CLml/h/kg5821196191588196117061407250
Apparent Vdml/kg10,37712,389653910,7231146654256324947
thalf, brainh13.925.7a2.6910.50.7514.2a2.2710.6
AUClast, plasmah*ng/ml98573448682610015766452230
S.E._AUClast, plasmah*ng/ml23.380.627.779.239.654.643.761.3
AUClast, brainh*ng/ml65.318682850562.42066381416
S.E._AUClast, brainh*ng/ml2.203.3560.824.08.213.8531.995.0
  • Apparent CL, apparent clearance (CL/F); Apparent Vd, apparent volume of distribution (Vd/F); AUClast, brain, area under the curve from zero to the time of last measured concentration in brain; AUClast, plasma, area under the curve from zero to the time of last measured concentration in plasma; S.E._AUClast, brain, standard error of an estimate of area under the curve in brain; S.E._AUClast, plasma, standard error of an estimate of area under the curve in plasma; thalf, half-life of a drug in plasma; thalf, brain, half-life of a drug in brain.

  • a The half-life was determined by the slope of last three time points in concentration-time profile.