Sinmyo K, Hosoi H, Suwa H, Kitagawa M, Yamaguchi K, Susaki H
Dept. of Surgery, Yokosuka Kyosai Hospital.
Gan To Kagaku Ryoho. 1989 May;16(5):2051-7.
The influence of OK-432 on the activation of UFT, consisting of tegafur and Uracil, was examined in patients with gastric cancer and colonic cancer. In 14 gastric cancer and 15 colonic cancer cases, to which UFT 400 mg/day and OK-432 2KE 2/W were administered orally and intra-muscularly for 2 weeks preoperatively until surgical treatment, intratumor 5-fluorouracil (5-FU) concentration was measured and compared with that of patients who given UFT 400 mg/day orally for 2 weeks (15 gastric cancer and 15 colonic cancer cases). As the results, in the groups of patients given OK-432, the concentration in gastric cancer tissue was 0.093 +/- 0.067 microgram/g and that in colonic cancer was 0.098 +/- 0.058 microgram/g. Both values exceeded 0.05 microgram/g which is considered to be the effective intratumor 5-FU concentration. No difference was observed in these cases given UFT alone. The ratio of intratumor 5-FU concentration vs. that of normal tissue was 2.5 for gastric cancer and 2.7 for colonic cancer and the ratio of tumor vs. serum 5-FU concentrations was 8.5 for gastric cancer and 10.9 for colonic cancer. No difference was also observed in these values in cases given UFT alone. From above results, it seemed that the clinical dose of OK-432 2KE 2/W had no influence on the activation of UFT, so that the combination therapy of UFT and OK-432 was found to be clinically useful.
在胃癌和结肠癌患者中研究了溶链菌制剂(OK-432)对由替加氟和尿嘧啶组成的优福定(UFT)激活的影响。在14例胃癌和15例结肠癌患者中,术前2周每天口服400mg UFT并每周2次肌肉注射2KE OK-432,直至进行手术治疗,测量肿瘤内5-氟尿嘧啶(5-FU)浓度,并与每天口服400mg UFT 2周的患者(15例胃癌和15例结肠癌患者)进行比较。结果显示,给予OK-432的患者组中,胃癌组织中的浓度为0.093±0.067微克/克,结肠癌中的浓度为0.098±0.058微克/克。这两个值均超过了被认为是有效的肿瘤内5-FU浓度的0.05微克/克。仅给予UFT的这些病例中未观察到差异。胃癌肿瘤内5-FU浓度与正常组织浓度之比为2.5,结肠癌为2.7,肿瘤与血清5-FU浓度之比,胃癌为8.5,结肠癌为10.9。仅给予UFT的病例中这些值也未观察到差异。从上述结果来看,似乎临床剂量的每周2次2KE OK-432对UFT的激活没有影响,因此发现UFT与OK-432的联合治疗在临床上是有用的。