TABLE 1

Pharmacokinetic parameters (mean ± S.D.) of erlotinib, active metabolite M14, and total radioactivity after a single100-mg oral dose of [14C]erlotinib to male volunteers (n = 4)


Parameter

Erlotinib

M14

Total 14Ca
Cmax (μg/ml) 1.39 ± 0.39 0.07 ± 0.03 1.40 ± 0.47
tmax (h) 1.4 ± 1.0 1.1 ± 1.0 1.1 ± 1.0
AUC0-last (μg · h/ml) 14.4 ± 5.4 0.5 ± 0.3 11.8 ± 4.8
AUC0-∞ (μg · h/ml) 14.8 ± 5.3 0.7 ± 0.4 14.7 ± 6.3
t½ (h)
8.1 ± 3.5
7.7 ± 4.3
10.0 ± 5.0
  • a Total 14C is expressed in μg-Eq erlotinib per ml.