Unit | AEE788 | Afatinib | AZD3759 | Dacomitinib | Erlotinib | Gefitinib | Osimertinib | Vandetanib | |
---|---|---|---|---|---|---|---|---|---|
thalf | h | 17.6 | 5.95 | 2.75 | 8.99 | 0.846 | 4.20 | 2.24 | 5.74 |
Apparent CL | ml/h/kg | 531 | 679 | 1598 | 822 | 1570 | 1431 | 1657 | 614 |
Apparent Vd | ml/kg | 13,502 | 5827 | 6349 | 10,667 | 1916 | 8680 | 5353 | 5085 |
thalf, brain | h | 5.1 | 10.5 | 2.32 | 16.6 | 0.95 | 4.76 | 3.59 | 41.8a |
AUClast, plasma | h*ng/ml | 858 | 1279 | 617 | 877 | 609 | 658 | 566 | 1442 |
S.E._AUClast, plasma | h*ng/ml | 61.8 | 234 | 95.9 | 135 | 49.7 | 95.3 | 81.6 | 98.7 |
AUClast, brain | h*ng/ml | 1599 | 3082 | 1633 | 8572 | 124 | 1449 | 8913 | 10,773 |
S.E._AUClast, brain | h*ng/ml | 89.1 | 174 | 72.0 | 307 | 6.12 | 57.0 | 1584 | 563 |
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, brain, half-life of a drug in brain; thalf, half-life of a drug in plasma.
↵a The half-life was determined by the slope of last three time points in concentration-time profile.