摘要
目的:前列腺特异性膜抗原(prostate specific membrane antigen,PSMA)可作为前列腺癌诊断的重要靶点。该研究成功制备了1种新型68Ga标记PSMA小分子抑制剂PSMA11,并根据《中华人民共和国药典》标准进行质量控制,同时探讨该分子影像探针在前列腺癌动物模型中的靶向显像效果。方法:利用68Ge/68Ga发生器淋洗产生68Ga液,标记PSMA11制备正电子分子探针68Ga-PSMA11;建立符合药典标准的质量标准草案,对药品进行质量控制;利用小动物PET/CT,在人前列腺癌细胞LNCaP的SCID小鼠移植瘤模型上研究68Ga-PSMA11在注射后体内动态分布情况。结果:成功制备获得68GaPSMA11,质量控制符合规定,放射化学纯度大于99%,其在体内除肾脏及膀胱放射性生理性高分布外,在肿瘤部位有较明显特异性浓聚,其余器官组织放射性分布均处于较低水平。结论:68Ga-PSMA11标记方法简便,在体内肿瘤中特异性摄取程度高,是一个理想的正电子型PSMA特异性分子探针。
Objective: Prostate specific membrane antigen (PSMA) plays an important role in diagnosis of prostate cancer. In this study, researchers labeled a new type PSMA inhibitor PSMA11 with 68Ga, did quality control (QC) according to Chinese Pharmacopoeia, and investigated pharmaceutical effect in prostate cancer animal models. Methods: Positron molecular probe 68Ga- PSMA11 prepared by PSMA11 precursor labeling with 68Ga, which was eluted from 68Ge/68Ga generator. Quality criterion according to standard of pharmacopoeia was established for QC of 68Ga-PSMA11. And the probe was injected into mice of LNCaP xenograft model for dynamic imaging by small animal PET/CT. Results: 68Ga-PSMA11 was successfully prepared, and QC was in compliance with quality criterion. Radiochemical purity was greater than 99%. The probe was combined with tumor specifically, besides physiological distribution in kidneys and bladder. Conclusion: 68Ga-PSMA11 was easy to label and had high intake in tumor. It is a promising positron molecular probe targeting PSMA.
作者
张骥
许晓平
刘成
张建平
罗建民
刘畅
胡四龙
宋少莉
章英剑
ZHANG Ji;XU Xiaoping;LIU Cheng;ZHANG Jianping;LUO Jianmin;LIU Chang;HU Silong;SONG Shaoli;ZHANG Yingjian(Department of Nuclear Medicine,Fudan University Shanghai Cancer Center,Department of Oncology,Shanghai Medical College,Fudan University,Shanghai 200032, China;Department of Nuclear Medicine,Shanghai Proton and Heavy Ion Center,Shanghai 201315,China;Center for Biomedical Imaging,Fudan University,Shanghai 200032,China;Shanghai Engineering Research Center of Molecular Imaging Probes,Shanghai 200032,China;Key Laboratory of Nuclear Physics and Ion-beam Application, Fudan University,Shanghai 200433,China)
出处
《肿瘤影像学》
2019年第4期209-215,共7页
Oncoradiology
基金
上海分子影像探针工程技术研究中心项目(14DZ2251400)
