Table 1.

Pharmacokinetic and pharmacodynamic studies of capecitabine in combination with TAS-114 or gimeracil

PlasmaTumor
5-FUTAS-114Free FdUMPdUMPFree TS (pmol/mg protein)
2 hours after administration
DrugsDose (mg/kg)AUC0-6 (ng·h/mL)AUC0-6 (ng·h/mL)AUClast (pmol·h/g tissue)AUClast (nmol·h/g tissue)MeanSD
Nontreatment0.7390.086
Capecitabine2401092,8994300.0500.006
5395217,1175260.0220.005
8091,16112,5485940.0130.005
Capecitabine/TAS-114240/384505,4152,0922780.0420.011
240/1501,34528,3621,3461720.0660.009
240/6001,91781,046789690.0570.013
Capecitabine/gimeracil240/0.182,2474,2734540.0330.016
240/0.72,4696,2285440.0220.006
  • NOTE: Plasma and tumor tissues were collected at 0.5, 1, 2, 4, and 6 hours after drug administration from three nude mice with MX-1 (human breast cancer) at each sampling point per group.