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Lu-FAPI-4
- Development stage
- Unknown
- Lead developer
- German Cancer Research Center
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous
01
Overview
Lu-FAPI-4 (lutetium Lu 177 FAPI-4) is a therapeutic radiopharmaceutical consisting of the fibroblast activation protein (FAP) inhibitor FAPI-04 conjugated to the beta-emitting radionuclide lutetium-177 (177Lu) via a DOTA chelator. Developed by the German Cancer Research Center (DKFZ) and Heidelberg University Hospital, Lu-FAPI-4 selectively targets fibroblast activation protein alpha (FAPα), which is highly overexpressed on cancer-associated fibroblasts (CAFs) within the tumor stroma of over 90% of epithelial carcinomas. Upon binding to FAP, the radioligand is internalized, delivering localized beta radiation that induces DNA damage and cell death in both CAFs and neighboring tumor cells. Lu-FAPI-4 has been investigated in preclinical and early-phase clinical studies for the treatment of various solid tumors, including breast, colon, pancreatic, and lung cancers, as well as inflammatory conditions like rheumatoid arthritis.
- Other names
- [177Lu]Lu-FAPI-04[177Lu]Lu-FAPI-4lutetium (177Lu) FAPI-4lutetium Lu 177 FAPI-04lutetium Lu 177 FAPI-4
02
Targets
FAP (Fibroblast activation protein alpha)
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