FAP-targeting radiopharmaceuticals

FAP-targeting radiopharmaceuticals represent a rapidly evolving class of theranostic agents designed to target fibroblast activation protein alpha (FAP). FAP is a transmembrane serine protease that is highly overexpressed on cancer-associated fibroblasts (CAFs) within the tumor microenvironment of over 90% of epithelial solid tumors, while remaining virtually absent in healthy adult tissues. This class of agents utilizes FAP-targeting ligands (which can be small molecules, cyclic peptides, or monoclonal antibodies) conjugated to chelators that bind radioactive isotopes. For diagnostic imaging (PET/SPECT), isotopes such as Gallium-68 ($^{68}\text{Ga}$) or Fluorine-18 ($^{18}\text{F}$) are employed to visualize tumor boundaries and metastases with high tumor-to-background contrast. For therapeutic applications (radiotherapy/radioligand therapy), beta-emitters like Lutetium-177 ($^{177}\text{Lu}$) or alpha-emitters like Actinium-225 ($^{225}\text{Ac}$) are used to deliver localized, cytotoxic radiation directly to the tumor stroma, inducing DNA double-strand breaks and destroying the supportive tumor microenvironment.

Other names

FAP-targeted radioligand therapyFAP-targeted radionuclide therapyFAP-targeted radiopharmaceuticalsFAP-targeting radioligand therapyFAP-targeting radionuclide therapyFAP-targeting radiopharmaceuticals