结直肠癌的靶向治疗药物研究进展

王政, 邹建军, 李哲, 沈素, 余俊先

中国药学杂志 ›› 2016, Vol. 51 ›› Issue (24) : 2077-2081.

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中国药学杂志
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中国药学杂志 ›› 2016, Vol. 51 ›› Issue (24) : 2077-2081. DOI: 10.11669/cpj.2016.24.001
消化道肿瘤药物的研发与临床应用专栏

结直肠癌的靶向治疗药物研究进展

  • 王政1, 邹建军2, 李哲1, 沈素1, 余俊先1*
作者信息 +

Targeted Drugs in Colorectal Cancer

  • WANG Zheng1, ZOU Jian-jun2, LI Zhe1, SHEN Su1, YU Jun-xian1*
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文章历史 +

摘要

结直肠癌是常见的消化道肿瘤,多数患者在确诊时已属于中晚期,化疗+靶向药物治疗能有效提高患者的中位生存期。已上市的靶向药物分为两类,单克隆抗体和小分子激酶抑制剂,前者有贝伐珠单抗、西妥昔单抗、帕尼单抗、雷莫芦单抗,后者包括瑞戈非尼、阿柏西普。根据药物的机制分类,贝伐珠单抗和帕尼单抗作用于肿瘤细胞表皮生长因子受体(EGFR),其余4个作用于肿瘤新生血管内皮生长因子(VEGF)及其受体(VEGFR)。目前,我国药企自主研发的阿帕替尼、法米替尼用于结直肠癌的Ⅲ期临床试验也在紧密进行中。然而结直肠癌靶向治疗所面临的耐药性和毒性反应亦不容忽视。未来的努力方向是研究发现新靶点、新药物,例如PD-1抑制剂可能为结直肠癌患者带来新的生机。

Abstract

Colorectal cancer is a common gastrointestinal cancer which always diagnosed too late. However, nowadays the median survival of patients has been effectively improved by chemotherapy plus targeted therapy. Targeted drugs on the market can be divided into two categories, monoclonal antibodies and small molecule kinase inhibitors(TKI). Bevacizumab, cetuximab, panitumumab, ramucirumab are monoclonal antibody. TKIs are as followed:regorafenib, ziv-aflibercept.According to the drug mechanism, bevacizumab and panitumumab target at epidermal growth factor receptor(EGFR)on tumor cells. While the remaining four drugs target at vascular endothelial growth factor(VEGF) and its receptor(VEGFR). Clinical trials of Chinese domestic drugs apatinib and famitinib are undergoing. Currently, the main issue of colorectal cancer targeted therapy is how to overcome drug resistance and reducetoxicity. The direction of future work is finding new targets, new drugs in colorectal cancer, such as PD-1 inhibitors which may bring new vitality to worldwide patients.

关键词

结直肠癌 / 靶向药物 / 表皮生长因子受体 / 血管内皮生长因子 / 血管内皮生长因子受体

Key words

colorectal cancer / targeted drug / epidermal growth factor receptor / vascular endothelial growth factor / vascular endothelial growth factor receptor

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王政, 邹建军, 李哲, 沈素, 余俊先. 结直肠癌的靶向治疗药物研究进展[J]. 中国药学杂志, 2016, 51(24): 2077-2081 https://doi.org/10.11669/cpj.2016.24.001
WANG Zheng, ZOU Jian-jun, LI Zhe, SHEN Su, YU Jun-xian. Targeted Drugs in Colorectal Cancer[J]. Chinese Pharmaceutical Journal, 2016, 51(24): 2077-2081 https://doi.org/10.11669/cpj.2016.24.001
中图分类号： R965   

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基金

国家重大新药创制专项(2010ZX09401-301)
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