Table 2.

PD model variables of gefitinib corresponding to pERK inhibition in LN229-wild-type EGFR and LN229-EGFRvIII mutant tumors following 10 mg/kg i.v., 50 mg/kg i.a., or 150 mg/kg p.o. single-dose administrations

VariablesLN229-wild-type EGFR tumor
LN229-EGFRvIII mutant tumor
10 mg/kg i.v.50 mg/kg i.a.150 mg/kg p.o.10 mg/kg i.v.50 mg/kg i.a.150 mg/kg p.o.
IC50 (μg/g)12.1 (42.6)*20.1 (33.8)27.5 (31.4)6.8 (26.8)11.4 (23.6)17.3 (16.9)
Kin (h−1)3.6 (18.9)6.6 (8.9)3.4 (13.8)5.1 (18.9)5.7 (13.3)5.1 (15.6)
Kout (h−1)3.3 (16.7)7.8 (7.8)3.8 (12.8)5.4 (17.2)7.1 (7.0)4.5 (14.5)
Ktr (h−1)0.92 (20.5)0.34 (12.0)0.17 (11.2)1.18 (18.8)0.12 (19.7)0.037 (21.9)
  • * Values represent mean (% coefficient of variation) of model fitted variables.