[177Lu]FAPI-46

[177Lu]FAPI-46 is a theranostic radiopharmaceutical consisting of a quinoline-based fibroblast activation protein inhibitor (FAPI) ligand, FAPI-46, labeled with the beta-emitting radionuclide lutetium-177 ($^{177}$Lu). It specifically targets fibroblast activation protein (FAP), an enzyme highly expressed on the surface of cancer-associated fibroblasts (CAFs) within the tumor stroma of various epithelial malignancies, including pancreatic, breast, and lung cancers. Upon binding to FAP, the compound delivers localized beta radiation to the tumor microenvironment. This radiation induces DNA damage and cell death not only in the targeted CAFs but also in adjacent tumor cells through the "cross-fire effect," which is facilitated by the relatively long tissue range of beta particles compared to alpha particles. The drug is designed to exploit the high tumor-to-background ratio provided by FAP expression for both imaging (when labeled with diagnostic isotopes) and targeted radionuclide therapy.

Other names

Lutetium (177Lu) FAPI-46177Lu-labeled FAPI-46[177Lu]Lu-FAPI-46