Kuyumcu Serkan, Sanli Yasemin, Subramaniam Rathan M
Department of Nuclear Medicine, Istanbul Faculty of Medicine, Istanbul University, Istanbul, Turkey.
Otago Medical School, University of Otago, Dunedin, New Zealand.
Front Oncol. 2021 Nov 11;11:758958. doi: 10.3389/fonc.2021.758958. eCollection 2021.
Fibroblast activation protein (FAP), overexpressed on cancer-associated fibroblasts (CAFs), is a novel target for molecular imaging of various tumors. Recently, the development of several small-molecule FAP inhibitors for radiolabeling with Ga has resulted in the emergence of studies evaluating its clinical role in cancer imaging. Preliminary findings have demonstrated that, in contrast to radiotracers taking advantage of cancer-specific targets such as PSMA and DOTATATE, FAPs as a target are the most promising that can compete with FDG in terms of widespread indications. They also have the potential to overcome the shortcomings of FDG, particularly false-positive uptake due to inflammatory or infectious processes, low sensitivity in certain cancer types, and radiotherapy planning. In addition, the attractive theranostic properties may facilitate the treatment of many refractory cancers. This review summarizes the current FAP variants and related clinical studies, focusing on radiopharmacy, dosimetry, and diagnostic and theranostic applications.
成纤维细胞活化蛋白(FAP)在癌症相关成纤维细胞(CAF)上过度表达,是各种肿瘤分子成像的新靶点。最近,几种用于用镓进行放射性标记的小分子FAP抑制剂的开发,导致了评估其在癌症成像中临床作用的研究出现。初步研究结果表明,与利用癌症特异性靶点(如PSMA和DOTATATE)的放射性示踪剂相比,FAP作为靶点在广泛适应症方面最有希望与FDG竞争。它们还有潜力克服FDG的缺点,特别是由于炎症或感染过程导致的假阳性摄取、某些癌症类型中的低敏感性以及放射治疗计划。此外,有吸引力的诊疗特性可能有助于治疗许多难治性癌症。本综述总结了当前的FAP变体及相关临床研究,重点关注放射性药物学、剂量学以及诊断和诊疗应用。