Department of Nuclear Medicine, Medical Faculty and University Hospital Duesseldorf, Heinrich-Heine-University Duesseldorf, Moorenstrasse 5, 40225, Duesseldorf, Germany.
Department of Nuclear Medicine, Heidelberg University Hospital, Im Neuenheimer Feld 400, 69120 Heidelberg, Germany.
PET Clin. 2023 Jul;18(3):419-428. doi: 10.1016/j.cpet.2023.02.007. Epub 2023 Apr 6.
Fibroblast activation protein (FAP)-targeted radioligand therapy offers a possibility of a novel cancer therapeutic strategy, aiming at tumor stroma1. Early clinical translations of FAP-tracers occurred as early as in the 1990s using antibodies, without substantial achievement further than the clinical phase II trial. The essential step toward the theranostic approach, with a conceptual combination of diagnostic and therapeutic emitters in a specific tracer, began with the implementation of small-molecule FAP-enzyme inhibitors (FAPI) in 2018. Currently, FAPI-04 and FAPI-46, containing DOTA-chelators with the possibility of radionuclide combination (Ga-68, Y-90, and Lu-177), are the compounds most widely used in the theranostic regimen.
成纤维细胞激活蛋白（FAP）靶向放射性配体治疗为肿瘤基质¹提供了一种新的癌症治疗策略。早在 20 世纪 90 年代，就使用抗体进行了 FAP 示踪剂的早期临床转化，但除了临床二期试验外，没有取得实质性进展。治疗方法的关键步骤是在特定示踪剂中概念性地结合诊断和治疗发射体，这始于 2018 年小分子 FAP 酶抑制剂（FAPI）的实施。目前，含有 DOTA 螯合剂且有可能与放射性核素（Ga-68、Y-90 和 Lu-177）结合的 FAPI-04 和 FAPI-46 是治疗方案中最广泛使用的化合物。
