The antitumor effects of UFT and UFT/LV against Co-3 tumor xenografts, as well as the effects of the maximum tested doses of UFT and leucovorin, administered alone or in combination, against Co-3 human colon cancer xenografts are shown. BALB/c-nu/nu mice (n=6/group) were implanted subcutaneously with Co-3 cancer fragments and the treatments were initiated when the mice had tumors of 100–130 mm3. Leucovorin (10 mg/kg/day, ▵) and UFT (20 mg/kg/day, ●) were administered orally on a qd x 14 schedule either alone or in combination (▴). The changes in mean tumor volume were recorded over time and are expressed as the mean ± SD. **Significantly different from the UFT 20 mg/kg/day group at p<0.01 (Student’s t-test). Dotted line, RTV10.