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.

中文翻译：

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成纤维细胞活化蛋白-α放射性药物的开发：最新进展和展望


成纤维细胞激活蛋白-α（FAP）由于其在癌症相关成纤维细胞（CAF）和其他涉及纤维化和炎症的病理状况中选择性表达，已成为放射性药物领域的一个有前途的靶标。最近的进展集中在开发用于诊断成像和靶向放射性核素治疗的 FAP 特异性放射性配体。该观点总结了 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，我们还分析了FAP靶向放射性药物的优势和存在的问题，并探讨了该靶点的重点突破方向，以促进FAP靶向放射性药物的开发和转化。