Beijing Institute of Brain Disorders, Laboratory of Brain Disorders, Ministry of Science and Technology, Collaborative Innovation Center for Brain Disorders, Capital Medical University, Beijing, 100069, China.
Department of Nuclear Medicine, Beijing Tiantan Hospital, Capital Medical University, Beijing, 100070, China.
Eur J Med Chem. 2024 Nov 5;277:116787. doi: 10.1016/j.ejmech.2024.116787. Epub 2024 Aug 27.
Fibroblast activation protein-α (FAP) has emerged as a promising target in the field of radiopharmaceuticals due to its selective expression in cancer-associated fibroblasts (CAFs) and other pathological conditions involving fibrosis and inflammation. Recent advancements have focused on developing FAP-specific radioligands for diagnostic imaging and targeted radionuclide therapy. This perspective summarized the latest progress in FAP radiopharmaceutical development, highlighting novel radioligands, preclinical evaluations, and potential clinical applications. Additionally, we analyzed the advantages and existing problems of targeted FAP radiopharmaceuticals, and discussed the key breakthrough directions of this target, so as to improve the development and conversion of FAP-targeted radiopharmaceuticals.
成纤维细胞激活蛋白-α（FAP）因其在癌相关成纤维细胞（CAFs）和其他涉及纤维化和炎症的病理状况中的选择性表达，已成为放射性药物领域有前途的靶点。最近的进展集中在开发 FAP 特异性放射性配体用于诊断成像和靶向放射性核素治疗。本综述总结了 FAP 放射性药物开发的最新进展，重点介绍了新型放射性配体、临床前评估和潜在的临床应用。此外，我们分析了靶向 FAP 放射性药物的优势和存在的问题，并讨论了该靶点的关键突破方向，以提高 FAP 靶向放射性药物的开发和转化。
