Table 1.

Summary of pharmacokinetic variables for erlotinib and OSI-420

VariableDay 1 (CV%)Day 8 (CV%)Day 34 (CV%)
CL (L/h/m2)37.9 (4)23.7 (5)25.9 (6)
Ka (h−1)0.94 (43)0.24 (59)0.17 (145)
Ke (h−1)0.29 (52)0.49 (72)0.29 (142)
Kemet (h−1)3.96 (52)4.07 (71)3.46 (141)
Tau gut (h)1.05 (14.4)0.74 (21)0.0 (Fixed)
Tau CSF (h)1.37 (Fixed)
K23 (h−1)1.02 × 10−4
K32 (h−1)6.00
K45 (h−1)0.98 × 10−4
K54 (h−1)4.79
V (L/m2)13.1 (52)4.87 (73)9.02 (145)
VCSF (L/m2)0.023 Fixed
Erlotinib AUC0-24 (ng·h/mL)19,41232,851Plasma, 30,365; CSF, 2,129
OSI-420 AUC0-24 (ng·h/mL)1,4163,921Plasma, 2,527; CSF, 240
Erlotinib AUC0-24 (ng·h/mL), NCAPlasma, 28,388; CSF, 1,949
OSI-420 AUC0-24 (ng·h/mL), NCAPlasma, 2,425; CSF, 209
  • Abbreviations: CV, coefficient of variation; NCA, noncompartmental analysis; CL, oral clearance.