Yoshiya N, Adachi S, Misawa Y, Ishida M, Yuzawa H, Kanazawa K, Takeuchi S
Dept. of Obstetrics and Gynecology, School of Medicine, Niigata University.
Gan To Kagaku Ryoho. 1988 Feb;15(2):285-9.
Antitumor effects of UFT, tegafur (FT-207), cisplatin (CDDP) and the combination of UFT with CDDP on a human ovarian cancer xenograft in nude mice and the concentration of 5-FU in the tumor tissue and major organs were studied. UFT (48.6mg/kg/day X 20) or tegafur (15.0mg/kg/day X 20) was daily administrated orally, and CDDP (5mg/kg/day X 3) was administrated intraperitoneally at an 7-day interval. The inhibition rates of the tumor growths were 49.6% with UFT, -2.3% with tegafur and 17.7% with CDDP, respectively. In the combination of UFT with CDDP, severe side effect were observed. The concentration of 5-FU in UFT-treated group was higher than tegafur group: about 2 times in the tumor, 5 times in the liver, 9 times in the kidney and 4 times in the spleen, respectively. In the combination of UFT with CDDP, the concentration of 5-FU in major organs, especially in the kidney, in nude mice that died at 10 day after drug administration were higher than in those of UFT. These findings indicate that UFT increases the intratumoral concentration of 5-FU to elicit better antitumor effect and also the concentration of 5-FU in various normal organs after long time administration.
研究了优福定（UFT）、替加氟（FT - 207）、顺铂（CDDP）以及UFT与CDDP联合用药对裸鼠人卵巢癌异种移植瘤的抗肿瘤作用，以及肿瘤组织和主要器官中5 - 氟尿嘧啶（5 - FU）的浓度。优福定（48.6mg/kg/天×20天）或替加氟（15.0mg/kg/天×20天）每日口服给药，顺铂（5mg/kg/天×3天）每隔7天腹腔注射给药。肿瘤生长抑制率分别为：优福定49.6%、替加氟 - 2.3%、顺铂17.7%。在UFT与CDDP联合用药时，观察到严重的副作用。UFT治疗组肿瘤组织中5 - FU的浓度高于替加氟组：肿瘤中约高2倍，肝脏中高5倍，肾脏中高9倍，脾脏中高4倍。在UFT与CDDP联合用药时，给药后10天死亡的裸鼠主要器官尤其是肾脏中5 - FU的浓度高于UFT组。这些结果表明，优福定可提高肿瘤组织中5 - FU的浓度以产生更好的抗肿瘤效果，且长期给药后还可提高各正常器官中5 - FU的浓度。
