药学学报, 2012, 47(10): 1297-1305
引用本文:
汤 沁, 丁 倩, 林 莉, 张珍珍, 代 争, 詹金彪. 针对HER2靶点的抗体药物研究与肿瘤靶向治疗[J]. 药学学报, 2012, 47(10): 1297-1305.
TANG Qin, DING Qian, LIN Li, ZHANG Zhen-zhen, DAI Zheng, ZHAN Jin-biao. Development of antibody drugs targeting against HER2 for cancer therapy[J]. Acta Pharmaceutica Sinica, 2012, 47(10): 1297-1305.

针对HER2靶点的抗体药物研究与肿瘤靶向治疗
汤 沁, 丁 倩, 林 莉, 张珍珍, 代 争, 詹金彪*
(浙江大学医学院生物化学系, 浙江 杭州 310058)
摘要:

人类表皮生长因子受体2 (HER2) 属于跨膜酪氨酸激酶受体家族的成员, 在肿瘤细胞中存在过表达。研究显示在乳腺癌、卵巢癌、胃癌、肺癌、前列腺癌中均存在不同程度的HER2过表达。抗体靶向治疗与传统化疗相比, 特异性强, 毒副作用小。本文介绍了曲妥珠单抗和帕妥珠单抗的单药治疗效果和与化疗药物、激素治疗、疫苗的联合治疗效果, 以及偶联药物策略, 阐述了其他新型抗HER2抗体药物, 特别是双特异抗体、免疫毒素以及抗体融合蛋白等研究近况, 为相应的HER2抗体药物开发和临床应用提供参考。

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Development of antibody drugs targeting against HER2 for cancer therapy
Abstract:

Human epidermal growth factor receptor 2 (HER2) belongs to the transmembrane glycoprotein receptor family.  Overexpression of HER2 could directly lead to tumorigenesis and metastasis.  This phenomenon could be observed in the breast cancer, ovarian cancer, gastric cancer, lung cancer and prostate cancer.  Compared with the conventional chemotherapy, the targeted treatment of antibody is more specific and has lower side effects.  This review describes the current status of monotherapy and combination therapies of anti-HER2 antibodies, trastuzumab and pertuzumab, with chemotherapeutic drugs.  The development trends of new formats of anti-HER2 antibody drugs such as bispecific antibody, immunotoxin are also discussed.

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