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去氧氟尿苷(Doxifluridine)是由瑞士Huffmann-La Roche开发,日本Roche公司生产,并于1987年在日本首次上市的新型尿嘧啶类抗肿瘤药。该药是氟尿嘧啶(5-FU)的前体药物。在肿瘤组织内受嘧啶核苷磷酸化酶的作用,转化成游离的氟尿嘧啶,从而抑制DNA、RNA的生物合成,显示其抗肿瘤作用。去氧氟尿苷的急性毒性较同类药低,在大鼠体内出现致畸作用。去氧氟尿苷的Ⅱ期临床试验表明:每日服800～1200mg,连续4W以上,有效率为:胃癌14.3%,结肠直肠癌9.2%,乳癌35.9%.肺癌无效。副作用主要为腹泻,白细胞减少,血小板减小,GOT、GPT上升。该药制成100～200mg的胶囊制剂,成
Doxifluridine is a new uracil-based antineoplastic agent developed by Huffmann-La Roche in Switzerland and produced by Roche in Japan and was first introduced in Japan in 1987. This drug is a prodrug of 5-fluorouracil. In the tumor tissue by the role of pyrimidine nucleoside phosphorylase, converted to free fluorouracil, thereby inhibiting DNA, RNA biosynthesis, showing its anti-tumor effect. The acute toxicity of doxifluridine is lower than that of other drugs, causing teratogenic effects in rats. Phase II clinical trial of doxifluridine showed that the daily effective dose was 800-1200mg for 4W and the effective rate was 14.3% for gastric cancer, 9.2% for colorectal cancer and 35.9% for breast cancer. Side effects mainly diarrhea, leukopenia, thrombocytopenia, GOT, GPT increased. The drug is made into 100 ~ 200mg capsules, into