5-氟尿嘧啶(5-fluorouracil,5-Fu)作为目前最广泛应用的细胞毒抗肿瘤药物之一,对结肠癌、乳腺癌、胃肠道癌、肝癌等癌症显示良好的治疗效果,但同时也伴随着很强的毒副作用,这一点严重限制了其临床应用。5-氟尿嘧啶高分子前药能够降低小分子5-Fu的毒副作用,增强抗肿瘤活性以及赋予其对肿瘤细胞的特殊亲和性。文章综述了近年来5-氟尿嘧啶高分子前药及其靶向抗肿瘤活性研究进展。
5-fluorouracil is one of the most widely used cytotoxic antitumor agents. It has been used in the carcinomas of colon, breast, gastrointestinal tract and liver. But its activity is also accompanied by strong side effects that had greatly limited its clinical applications. Polymeric prodrugs of 5-fluorouracil can reduce its toxicity, increase duration of antitumor activity and additionally, an affinity for tumor cells. In this review the research on polymeric prodrug of 5-fluorouracil and their targeting antitumor activities were reported.