Department of Medical Oncology, University of Texas, Southwestern Medical Center, Dallas, Texas 75390, USA.
Anticancer Drugs. 2011 Apr;22(4):311-6. doi: 10.1097/CAD.0b013e3283441a63.
5-Fluorouracil (5-FU) is the most widely used agent for the management of colorectal cancer. Capecitabine is metabolized by three enzymatic actions, the last of which is mediated by thymidine phosphorylase, to produce 5-FU. Given the oral bioavailability of capecitabine as well as in-vitro and in-vivo findings showing higher expression of thymidine phosphorylase in tumor cells and xenografts compared with normal tissue, capecitabine is an evolving candidate in the management of colorectal cancer with antimetabolite-based therapy. An ideal radiosensitizing agent must balance oncological outcomes with adverse effects and feasibility of administration. This discussion addresses the evolving role of 5-FU in the management of rectal cancer in the neoadjuvant setting in combination with ionizing radiation.
氟尿嘧啶（5-FU）是治疗结直肠癌最常用的药物。卡培他滨通过三种酶促作用代谢，最后一种由胸苷磷酸化酶介导，产生 5-FU。鉴于卡培他滨的口服生物利用度以及体外和体内研究发现，肿瘤细胞和异种移植物中的胸苷磷酸化酶表达高于正常组织，卡培他滨是一种具有代谢物基础的治疗结直肠癌的候选药物。理想的放射增敏剂必须在疗效、不良反应和给药可行性之间取得平衡。本文讨论了氟尿嘧啶在新辅助放疗联合治疗直肠癌中的作用。
