TABLE 3

Clinically observed and PBPK model–predicted pharmacokinetic parameters of crizotinib in healthy subjects following a single intravenous or oral administration of crizotinib

Data are expressed as geometric mean with percent coefficient of variation (CV%) in parentheses (n = 14 for the observed; n = 15 per group × 6 groups for the predicted).

Single Intravenous Infusion (50 mg)Single Oral Administration (250 mg)
CmaxAUC0–∞t1/2CmaxAUC0–∞t1/2
ng/mlng⋅h/mlhng/mlng⋅h/mlh
Observed155 (19)1067 (18)39 (16)100 (28)2321 (34)29 (10)
Predicted167 (11)1258 (23)45 (19)103 (34)2878 (47)58 (24)
P/Oa1.11.21.21.01.22.0
  • a Ratio of the predicted to observed results.