小分子酪氨酸激酶抑制剂在人表皮生长因子受体-2阳性乳腺癌中的应用进展  

Progress of small molecule tyrosine kinase inhibitors in human epidermal growth factor receptor-2 positive breast cancer

作　　者：肖琪 赵兵[1] XIAO Qi;ZHAO Bing(Department of Breast Medicine,the Third Clinical Medical College of Xinjiang Medical University,Xinjiang Uygur Autonomous Region,Urumqi 830011,China)

机构地区：[1]新疆医科大学第三临床医学院乳腺内科,新疆乌鲁木齐830011

出　　处：《中国当代医药》2024年第35期195-198,共4页China Modern Medicine

摘　　要：乳腺癌是女性最常见的恶性肿瘤,人表皮生长因子受体-2(HER-2)过表达是乳腺癌患者预后不良的独立因素。单克隆抗体类药物能显著改善HER-2阳性乳腺癌患者的结局,然而,大多数患者会产生单克隆抗体类药物耐药,小分子酪氨酸激酶抑制剂(TKI)一定程度上缓解了单克隆抗体耐药的现状。TKI通过抑制酪氨酸激酶生物活性,阻止酪氨酸残端磷酸化,抑制肿瘤细胞的损伤修复,诱导细胞凋亡,从多途径实现抗肿瘤效果。同时,TKI作为小分子化合物,具有跨越血脑屏障的能力,在脑转移的患者中也表现出良好的疗效。本文就已获批上市使用的HER-2阳性乳腺癌TKI的研究进展作一综述。Breast cancer is the most common malignant tumour in women,and human epidermal growth factor receptor-2(HER-2)overexpression is an independent factor for poor prognosis in breast cancer patients.The emergence of monoclonal antibody-based drugs can significantly improve the outcome of HER-2 positive breast cancer patients,however,most patients will inevitably develop resistance to monoclonal antibody-based drugs,and the introduction of small-molecule tyrosine kinase inhibitor(TKI)has alleviated the status quo of monoclonal antibody resistance to a certain extent.TKI is designed to inhibit the biological activity of tyrosine kinases by preventing the phosphorylation of tyrosine residues,inhibiting damage repair of tumour cells,and inducing the repair of tumour cell damage,as well as preventing the phosphorylation of tyrosine residues.It inhibits damage repair of tumour cells and induces apoptosis to achieve anti-tumour effect from multiple pathways.Moreover,TKI,as a small molecular compound with the ability to cross the blood-brain barrier,has shown good efficacy in patients with brain metastases.In this paper,we review the research progress of HER-2-positive breast cancer TKIs that have been approved for marketing use.

关 键 词：乳腺癌 人表皮生长因子受体-2 酪氨酸激酶抑制剂 靶向治疗 

分 类 号：R737.9[医药卫生—肿瘤]