Pharmaceutics (Feb 2024)

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

DOI
https://doi.org/10.3390/pharmaceutics16030345
Journal volume & issue
Vol. 16, no. 3
p. 345

Abstract

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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.

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