Beyond Small Molecules: Antibodies and Peptides for Fibroblast Activation Protein Targeting Radiopharmaceuticals
Xiaona Sun,
Yuxuan Wu,
Xingkai Wang,
Xin Gao,
Siqi Zhang,
Zhicheng Sun,
Ruping Liu,
Kuan Hu
Affiliations
Xiaona Sun
School of Printing and Packaging Engineer, Beijing Institute of Graphic Communication, Beijing 102600, China
Yuxuan Wu
School of Printing and Packaging Engineer, Beijing Institute of Graphic Communication, Beijing 102600, China
Xingkai Wang
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
Xin Gao
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
Siqi Zhang
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
Zhicheng Sun
School of Printing and Packaging Engineer, Beijing Institute of Graphic Communication, Beijing 102600, China
Ruping Liu
School of Printing and Packaging Engineer, Beijing Institute of Graphic Communication, Beijing 102600, China
Kuan Hu
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
Fibroblast activation protein (FAP) is a serine protease characterized by its high expression in cancer-associated fibroblasts (CAFs) and near absence in adult normal tissues and benign lesions. This unique expression pattern positions FAP as a prospective biomarker for targeted tumor radiodiagnosis and therapy. The advent of FAP-based radiotheranostics is anticipated to revolutionize cancer management. Among various types of FAP ligands, peptides and antibodies have shown advantages over small molecules, exemplifying prolonged tumor retention in human volunteers. Within its scope, this review summarizes the recent research progress of the FAP radiopharmaceuticals based on antibodies and peptides in tumor imaging and therapy. Additionally, it incorporates insights from recent studies, providing valuable perspectives on the clinical utility of FAP-targeted radiopharmaceuticals.