Table 5.

Comparison of pharmacokinetic variables between the oral and i.v. CI-1033 at the MTD and bioequivalent oral dose

VariableCanertinib-Cl-1033
I.v.
Oral
MTDMTDBioequivalent
Dose225500725
Kel0.2320.1570.157
t1/23.24.44.4
tmax0.42.32.3
Cmax2233265384
AUC3,5182,3853,458
VD3711,3361,336
CL73210210
F (%)3131
  • Abbreviations: Kel, elimination rate constant expressed in hours-1; t1/2, plasma half-life hours; tmax, time the maximum concentration occurs in hours; Cmax, maximum concentration expressed as ng/mL; AUC, area under the curve expressed as ng × Hr/mL; VD, volume of distribution expressed in liters (L); CL, clearance expressed as ng/h; F, fraction of drug absorbed expressed as a percentage.