Kaga F, Kitajima M, Ikeda Y, Seki M, Yagita A, Sohma S, Fukuzumi N
Gan To Kagaku Ryoho. 1982 Mar;9(3):489-95.
Thirty patients with gastric cancer were clinically studied by rectal administration of FT-207 suppository at a dose of 1500mg per day as a preoperative adjuvant chemotherapy. Eighteen of thirty patients were divided into two groups, 13 patients of which were only administrated with tegafur (FT-207) suppository (Group A) and 5 patients were administrated with glutathione (GSH) at a dose of 1200mg daily with FT-207 suppository (Group B): The tissue concentration of FT-207 and 5-FU in normal and cancer tissues was measured following the resection of the stomach. In addition, we studied anticancer effect of FT-207 suppository on the basis of our original pathological criteria. Experimental results revealed that 5-FU concentration in serum was reached to maximum at 3 to 4 hours following administration in both groups. The serum concentration in most cases of the former group was decreased to the lower level of the effective concentration for 8 hours, however the latter could be kept the effective concentration for more than 10 hours. The correlation between the tissue concentration and total dose was analyzed. 5-FU concentration, which was active substance of FT-207, in cancer tissue was higher than in normal one, especially in Borrmann II type cancer, but the difference of concentration was not found between group A and B. The correlation between total dose and anticancer effect was also analyzed. Histopathological effect in group A showed a mild change, such as necrosis of cancer nest. On the other hand, group B revealed a markedly effective change like scarring formation. As the result, administration of FT-207 suppository with GSH was clinically and histopathologically effective procedure as preoperative adjuvant chemotherapy.
对30例胃癌患者采用术前辅助化疗,经直肠给予FT - 207栓剂,剂量为每日1500mg,进行临床研究。30例患者中的18例分为两组,其中13例仅给予替加氟(FT - 207)栓剂(A组),5例在给予FT - 207栓剂的同时每日给予1200mg谷胱甘肽(GSH)(B组):胃切除术后测量正常组织和癌组织中FT - 207和5 - FU的组织浓度。此外,我们根据原有的病理标准研究了FT - 207栓剂的抗癌效果。实验结果显示,两组给药后3至4小时血清中5 - FU浓度均达到最高值。前一组大多数病例的血清浓度在有效浓度下限水平持续8小时,而后者可在有效浓度水平维持10小时以上。分析了组织浓度与总剂量之间的相关性。FT - 207的活性物质5 - FU在癌组织中的浓度高于正常组织,尤其是在Borrmann II型癌中,但A组和B组之间未发现浓度差异。还分析了总剂量与抗癌效果之间的相关性。A组的组织病理学效应表现为轻度变化,如癌巢坏死。另一方面,B组显示出明显有效的变化,如瘢痕形成。结果表明,FT - 207栓剂与GSH联合给药作为术前辅助化疗在临床和组织病理学上是有效的方法。