Watanabe K, Satoh H, Ohki S, Furue H, Komita T, Iketa T, Ikenaga M, Arimori S, Nagao T, Yamamoto S
Gan To Kagaku Ryoho. 1982 Apr;9(4):675-80.
Tumor regression was observed in only one patient. Twelve (33%) of the 36 patients reported adverse effects: gastrointestinal symptoms in 8, CNS symptoms in 3, and others in 1. The antitumor efficacy of TAC-278 was insufficient while incidence of adverse effects was similar to other 5-FU derivatives in man and the clinical usefulness of the drug was hardly found. TAC-278 has been developed with an aim to give higher plasma concentrations of 5-FU in man. Even at a dose causing adverse effects, however, the clinical efficacy of TAC-278 was unsatisfactory. The study is a meaning tal eince the results suggest that there might be a more important factor than blood concentration of 5-FU to enhance an antitumor effect of 5-FU derivatives.
仅在一名患者中观察到肿瘤消退。36名患者中有12名（33%）报告了不良反应：8例出现胃肠道症状，3例出现中枢神经系统症状，1例出现其他症状。TAC - 278的抗肿瘤疗效不足，而不良反应的发生率与其他5 -氟尿嘧啶衍生物在人体中的情况相似，几乎未发现该药物的临床实用性。开发TAC - 278的目的是使人血浆中的5 -氟尿嘧啶浓度更高。然而，即使在引起不良反应的剂量下，TAC - 278的临床疗效也不令人满意。该研究具有重要意义，因为结果表明，可能存在比5 -氟尿嘧啶血药浓度更重要的因素来增强5 -氟尿嘧啶衍生物的抗肿瘤作用。
