[Pharmacodynamic study on the effectiveness of UFT against cancer of gastro-intestinal (GI) tract]

Preoperative oral administration of either 5-FU 200 mg/day (15 patients) or UFT (tegafur plus uracil at a 1:4 molar ratio) 400 mg/day (22 patients) were carried out was carried out against the patients cancer of GI-tract 3 consecutive days till the morning of the operation. Serial blood samples of peripheral and portal veins were obtained for the measurement of concentration of 5-FU. The Concentration of 5-FU in normal and tumor tissues was measured in 13 patients given UFT pre-operatively. Thymidylate synthase inhibition rate were also measured in 5 of them. Furthermore, AgNOR count of tumor tissue before and after administration of UFT were examined in 11 patients. Following conclusions were obtained. (1) The Concentration of 5-FU in peripheral venous blood of UFT group was significantly higher than that of 5-FU group during 1-5 hrs after the last dose (p < 0.05). (2) The concentration of 5-FU in portal venous blood of 5-FU group was higher than that of UFT group during initial 2 hrs after the last dose. However, during 3 to 7 hrs after the last dose, UFT group showed a higher concentration. (3) In UFT group, the concentration of 5-FU in tumor tissue was significantly higher than that in normal tissue (p < 0.01). Consequently, preoperative administration of UFT can be effective for prevention of intraoperative prevention of hematogenous metastasis via portal system in cancer of gastrointestinal tract.