FAPI PET探针的开发及研究进展  

A review of the development and research progress of FAPI PET probes

作　　者：程华 白立言 宋少莉 CHENG Hua;BAI Liyan;SONG Shaoli(Department of Nuclear Medicine,Fudan University Shanghai Cancer Center,Department of Oncology,Shanghai Medical College,Fudan University,Shanghai 200032,China)

机构地区：[1]复旦大学附属肿瘤医院核医学科,复旦大学上海医学院肿瘤学系,上海200032

出　　处：《肿瘤影像学》2024年第5期485-492,共8页Oncoradiology

基　　金：国家自然科学基金(U23A20465)。

摘　　要：成纤维细胞活化蛋白(fibroblast activation protein,FAP)在癌症相关成纤维细胞(cancer-associated fibroblast,CAF)中的应用已引起核医学领域的广泛关注。FAP的高表达细胞存在于多数癌组织中,健康组织中很少表达,因此靶向FAP蛋白的核素探针有巨大的诊断和治疗潜力。与临床上广泛应用的18F-FDG相比,聚集于FAP的示踪剂在许多适应证中显示出更好的靶本底比值(肿瘤背景比值)。与18F-FDG不同,FAP靶向示踪剂的临床使用过程不需要复杂的准备工作,例如对患者的饮食限制,并且在治疗方法中提供了放射配体治疗的可能性。尽管早在20世纪90年代就有放射性标记抗体进行临床研究,但核医学中FAP靶向探针研发的突破性事件是2018年FAPI示踪剂的引入和临床应用。从那时起,靶向FAP示踪剂的开发和应用成为放射性制药和核医学界的热门话题,引起了制药公司的广泛关注。本文将针对FAP靶向放射性药物的开发和研究进展进行综述。The application of fibroblast activation protein(FAP)in cancer-associated fibroblast(CAF)has garnered widespread attention in nuclear medicine.FAP is highly expressed in most cancer tissues and rarely expressed in healthy tissues.Therefore,radionuclide probes targeting FAP have significant diagnostic and therapeutic potential.Compared to 18F-FDG,widely used in clinical practice,FAP-targeted tracers exhibit superior target-to-background ratio(tumor-to-background ratio)across various indications.Unlike 18F-FDG,the clinical use of FAP-targeted tracers does not require complex preparations like dietary restrictions for patients and offers the possibility of radioligand therapy(RLT).While radiolabeled antibodies have been studied clinically since the 1990s,the introduction and clinical application of FAPI tracers in 2018 marked a breakthrough event in the development of FAP-targeted probes within nuclear medicine.Since then,the development and application of targeted FAP tracers have become a hot topic among pharmaceutical companies as well as within the radiopharmaceutical and nuclear medicine communities.This article reviewed the current status and research progress of FAP-targeted radiopharmaceuticals.

关 键 词：成纤维细胞活化蛋白抑制剂 正电子发射体层成像/计算机体层成像探针 放射性探针 核医学显像 

分 类 号：R445.6[医药卫生—影像医学与核医学]