尽管基于5-氟尿嘧啶(5-FU)的化疗是结直肠癌的主要治疗方法,它有缺点,如全身毒性,缺乏有效性和选择性,和发展抵抗。卡培他滨,5-FU的前药形式,旨在克服这些缺点,为了满足更方便的治疗需求,为了提高安全性,通过肿瘤特异性转化为活性5-FU药物的耐受性和肿瘤内药物浓度水平。本综述的目的是提供5-FU疗法与卡培他滨之间的综合比较。在当前的审查中,讨论了抗癌药物的分类,并解释了卡培他滨从原始氟化类似物(5‑FU)的发展以克服其缺点。具体来说,5-FU与卡培他滨治疗的各种特性进行了比较,包括药物代谢,细胞机制,对细胞凋亡途径和细胞周期阶段的影响,安全性和耐受性。此外,讨论了卡培他滨活化为5-FU所需的三种代谢酶。卡培他滨,作为单一疗法或与其他化学疗法组合,表现出改善的药物疗效和生存率。然而,介导卡培他滨治疗化疗耐药的变化被归类为细胞内,细胞外或细胞表面因子,或细胞表型状态。未来的研究应该检查卡培他滨联合化疗药物以外的新型安全药物的疗效,这些药物在抑制肿瘤发生中起作用。进展和转移。
Although 5‑fluorouracil (5‑FU)‑based chemotherapy is the major treatment for colorectal cancer, it has disadvantages such as systemic toxicity, lack of effectiveness and selectivity, and development of resistance. Capecitabine, a prodrug form of 5‑FU, was designed to overcome these drawbacks, to fulfill the need for more convenient therapy, and to improve safety, tolerability and intratumor drug concentration levels through a tumor‑specific conversion to the active 5‑FU drug. The purpose of the present
review is to provide a comprehensive comparison between 5‑FU therapy and capecitabine. In the current
review, anticancer drug classification was discussed and the development of capecitabine from the original fluorinated analogue (5‑FU) to overcome its drawbacks was explained. Specifically, 5‑FU is compared with capecitabine therapy regarding various properties, including drug metabolism, cellular mechanism, effect on the apoptosis pathway and cell cycle phases, safety and tolerability. Moreover, three metabolizing enzymes required for the activation of capecitabine to 5‑FU were discussed. Capecitabine, as monotherapy or in combination with other chemotherapies, exhibited improved drug efficacy and survival. However, the changes that mediate the chemoresistance of capecitabine treatment were classified as intracellular, extracellular or cell surface factors, or cell‑phenotype state. Future studies should examine the efficacy of capecitabine combined with novel and safe drugs other than chemotherapeutic agents that play a role in the inhibition of tumor initiation, progression and metastasis.