FAPI-F1D

FAPI-F1D (also referred to as FAPI-46-F1D) is a dimeric small molecule targeting vector designed to bind fibroblast activation protein-alpha (FAP). Developed by researchers at the University Hospital Basel and Ulm University Medical Center, FAPI-F1D was engineered to address the rapid clearance and short tumor residence time characteristic of monomeric FAP inhibitors like FAPI-46. By dimerizing the FAP-binding quinoline moiety, the ligand achieves bivalent binding, which significantly enhances its affinity and prolongs retention within FAP-expressing cancer-associated fibroblasts in the tumor microenvironment. Preclinical evaluations, typically utilizing the lutetium-177 radiolabeled form ([177Lu]Lu-FAPI-F1D), have demonstrated high and specific tumor accumulation, making it a promising candidate for targeted radionuclide therapy (TRT) of solid tumors.

Other names

177Lu-FAPI-46-F1D177Lu-FAPI-F1D[177Lu]Lu-FAPI-46-F1D[177Lu]Lu-FAPI-F1D