Preprint Review Version 1 Preserved in Portico This version is not peer-reviewed

Beyond Small Molecules: Antibodies and peptides for Fibroblast Activation Protein Targeting Radiopharmaceuticals

Version 1 : Received: 5 February 2024 / Approved: 5 February 2024 / Online: 5 February 2024 (12:26:59 CET)

A peer-reviewed article of this Preprint also exists.

Sun, X.; Wu, Y.; Wang, X.; Gao, X.; Zhang, S.; Sun, Z.; Liu, R.; Hu, K. Beyond Small Molecules: Antibodies and Peptides for Fibroblast Activation Protein Targeting Radiopharmaceuticals. Pharmaceutics 2024, 16, 345. Sun, X.; Wu, Y.; Wang, X.; Gao, X.; Zhang, S.; Sun, Z.; Liu, R.; Hu, K. Beyond Small Molecules: Antibodies and Peptides for Fibroblast Activation Protein Targeting Radiopharmaceuticals. Pharmaceutics 2024, 16, 345.

Abstract

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 revolu-tionize 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, on tumor imaging and therapy. Additionally, it incorporates insights from recent studies, providing valuable perspectives on the clinical utility of FAP-targeted radiopharmaceuticals.

Keywords

FAP; Radiopharmaceuticals; PET Imaging; Theranostics; Radionuclide therapy

Subject

Medicine and Pharmacology, Medicine and Pharmacology

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