靶向HER2阳性肿瘤的PET/CT分子显像临床研究进展  

Progress in PET/CT Molecular Imaging Targeting HER2-positive Tumour

作　　者：周妮娜[1] 朱华[1] 杨志[1] ZHOU Ni’na;ZHU Hua;YANG Zhi(Key Laboratory of Carcinogenesis and Translational Research,Ministry of Education,Department of Nuclear Medicine,Peking University Cancer Hospital & Institute,Beijing 100142,China)

机构地区：[1]北京大学肿瘤医院暨北京市肿瘤防治研究所核医学科恶性肿瘤发病机制及转化研究教育部重点实验室,北京100142

出　　处：《肿瘤防治研究》2019年第4期376-381,共6页Cancer Research on Prevention and Treatment

摘　　要：人类表皮生长因子受体2(HER2)在多种肿瘤组织中均有不同程度表达,曲妥珠单抗,可明显提高HER2阳性乳腺癌、胃癌的总生存时间。目前对HER2过表达的检测方法主要是免疫组织化学染色和荧光原位杂交法,但这种有创性的检查不能作为肿瘤疗效评价的常规检查而多次进行。靶向HER2的PET/CT分子显像,有望实时、无创监测全身病灶的HER2表达情况。目前靶向HER2的PET/CT分子显像主要包括核素标记抗体显像、核素标记亲和体显像、核素标记抗体片段及纳米抗体显像。靶向HER2的PET/CT显像可用于监测全身病灶的HER2表达情况,监测HER2表达的异质性,可用于原发乳腺癌HER2阴性患者阳性转移灶的筛选,同时也可用于靶向治疗的疗效预测。长半衰期核素铜、锆(^(64)Cu、^(89)Zr)标记完整抗体可直接评估HER2结合Trastuzumab的情况,但其血液药代动力学较慢,血液清除率较慢,需较长时间点的显像,辐射剂量较高。短半衰期核素(^(68)Ga)标记亲和体显像、抗体片段及纳米抗体显像,由于其分子量小,生物分布快,注射药物后可短时间内显像(1～4 h),增加了患者的便利性,可重复显像,亲合体由于与抗体结合位点不同,可用于靶向治疗显像,另外其辐射剂量较低,可能更适于临床应用。Human epidermal growth factor receptor 2(HER2) is expressed in various tumors. Trastuzumab can significantly improve the overall survival time of HER2-positive breast cancer and gastric cancer patients.At present, the detection methods of HER2 overexpression are mainly IHC and FISH. However, this invasive examination can not be used as a routine examination. PET/CT molecular imaging targeting HER2 is expected to monitor the HER2 expression in whole-body lesions in real time and non-invasively. At present,PET/CT molecular imaging targeting HER2 mainly includes nuclide-labeled antibody imaging, nuclidelabeled affibody/antibody fragment/nanoantibody imaging. It can be used to monitor the expression and the heterogeneity of HER2, screen positive metastatic foci in patients with primary HER2-negative breast cancer and predict the curative effect. Long half-life nuclide(64Cu, 89Zr) labeled intact antibody can directly assess the situation of HER2 binding to trastuzumab, but its blood pharmacokinetics and blood clearance are slow,and long-time imaging is needed. In addition, the long half-life nuclides lead to higher radiation dose. Short half-life nuclide(68Ga) labeled affibody/antibody fragment/nanoantibody imaging, due to its small molecular weight, fast biological distribution and short-time imaging(1-4h) after the injection of drugs, can increase the convenience of the patients and be repeatedly imaged. As the binding site is different from antibody,affibody can be used for the imaging in target therapy. Also, the radiation caused by short half-life nuclide is significantly lower than that by long half-life nuclides, and may be more suitable for clinical application.

关 键 词：HER2 PET/CT 分子显像 靶向 

分 类 号：R817-3[医药卫生—影像医学与核医学] R730.40[医药卫生—放射医学]