Unit | AEE788 | Afatinib | AZD3759 | Dacomitinib | Erlotinib | Gefitinib | Osimertinib | Vandetanib | |
---|---|---|---|---|---|---|---|---|---|
thalf | h | 12.4 | 7.20 | 2.37 | 8.45 | 0.827 | 2.66 | 2.77 | 13.7 |
Apparent CL | ml/h/kg | 582 | 1196 | 1915 | 881 | 961 | 1706 | 1407 | 250 |
Apparent Vd | ml/kg | 10,377 | 12,389 | 6539 | 10,723 | 1146 | 6542 | 5632 | 4947 |
thalf, brain | h | 13.9 | 25.7a | 2.69 | 10.5 | 0.75 | 14.2a | 2.27 | 10.6 |
AUClast, plasma | h*ng/ml | 985 | 734 | 486 | 826 | 1001 | 576 | 645 | 2230 |
S.E._AUClast, plasma | h*ng/ml | 23.3 | 80.6 | 27.7 | 79.2 | 39.6 | 54.6 | 43.7 | 61.3 |
AUClast, brain | h*ng/ml | 65.3 | 186 | 828 | 505 | 62.4 | 206 | 638 | 1416 |
S.E._AUClast, brain | h*ng/ml | 2.20 | 3.35 | 60.8 | 24.0 | 8.21 | 3.85 | 31.9 | 95.0 |
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.