Lindner Thomas, Giesel Frederik L, Kratochwil Clemens, Serfling Sebastian E
Department of Nuclear Medicine, University Hospital Würzburg, 97080 Würzburg, Germany.
Department of Nuclear Medicine, University Hospital Düsseldorf, 40225 Düsseldorf, Germany.
Cancers (Basel). 2021 Nov 16;13(22):5744. doi: 10.3390/cancers13225744.
Targeting fibroblast activation protein (FAP) in cancer-associated fibroblasts (CAFs) has attracted significant attention in nuclear medicine. Since these cells are present in most cancerous tissues and FAP is rarely expressed in healthy tissues, anti-FAP tracers have a potential as pan-tumor agents. Compared to the standard tumor tracer [F]FDG, these tracers show better tumor-to-background ratios (TBR) in many indications. Unlike [F]FDG, FAP-targeted tracers do not require exhausting preparations, such as dietary restrictions on the part of the patient, and offer the possibility of radioligand therapy (RLT) in a theragnostic approach. Although a radiolabeled antibody was clinically investigated as early as the 1990s, the breakthrough event for FAP-targeting in nuclear medicine was the introduction and clinical application of the so-called FAPI-tracers in 2018. From then, the development and application of FAP-targeted tracers became hot topics for the radiopharmaceutical and nuclear medicine community, and attracted the interest of pharmaceutical companies. The aim of this review is to provide a comprehensive overview of the development of FAP-targeted radiopharmaceuticals and their application in nuclear medicine.
在癌症相关成纤维细胞（CAFs）中靶向成纤维细胞活化蛋白（FAP）已在核医学领域引起了广泛关注。由于这些细胞存在于大多数癌组织中，而FAP在健康组织中很少表达，抗FAP示踪剂具有作为泛肿瘤药物的潜力。与标准肿瘤示踪剂[F]FDG相比，这些示踪剂在许多适应症中显示出更好的肿瘤与本底比值（TBR）。与[F]FDG不同，靶向FAP的示踪剂不需要诸如患者饮食限制等繁琐的准备工作，并且在诊疗一体化方法中提供了放射配体治疗（RLT）的可能性。尽管早在20世纪90年代就对放射性标记抗体进行了临床研究，但核医学中靶向FAP的突破性事件是2018年所谓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药物和核医学领域的热门话题，并引起了制药公司的兴趣。本综述的目的是全面概述靶向FAP放射性药物的发展及其在核医学中的应用。
