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Capecitabine

卡培他濱

Mechanism of action:

Capecitabine 是一種氟嘧啶類(fluoropyrimidine carbamate)前驅藥,在體內會被轉化為活性代謝物 5-氟尿嘧啶(5-fluorouracil,5-FU)。由於腫瘤組織的胸腺嘧啶磷解酶(thymidine phosphorylase)的含量往往高於正常組織,因此 5-FU 在腫瘤組織中的生成比例可相對提高。隨後 5-FU 會再轉變成其他活性代謝物,如 FdUMP(5-fluoro-2'-deoxyuridine monophosphate),能抑制胸苷酸合成酶(thymidylate synthase),阻止 dTMP 合成; FUTP(5-fluorouridine triphosphate),摻入 RNA,干擾 RNA 功能與蛋白質合成;FdUTP,摻入 DNA,造成 DNA 異常,阻止癌細胞分裂與啟動細胞死亡相關路徑。

​Reference(s):

1. Walko CM et al. (2005). Capecitabine: a review. Clin Ther. 


2. Wagstaff AJ et al. (2003). Capecitabine: a review of its pharmacology and therapeutic efficacy in the management of advanced breast cancer. Drugs. 


3. Koukourakis GV et al. (2008). Efficacy of the oral fluorouracil pro-drug capecitabine in cancer treatment: a review. Molecules.

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