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Drug intelligence / Profile preview
177Lu-FAPI-RGD
- Development stage
- Phase 1
- Lead developer
- Peking Union Medical College Hospital
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules, Peptides
- Administration
- Intravenous
01
Overview
177Lu-FAPI-RGD is a dual-targeted radiopharmaceutical designed for the treatment of advanced or metastatic solid tumors. It is a heterodimeric molecule that combines a Fibroblast Activation Protein (FAP) inhibitor with an Arg-Gly-Asp (RGD) peptide motif. The FAP component targets tumor-associated fibroblasts (TAFs) within the tumor stroma, while the RGD motif targets integrin αvβ3, which is highly expressed on the surface of tumor cells and angiogenic endothelial cells. By binding to these two distinct markers in the tumor microenvironment, 177Lu-FAPI-RGD achieves high tumor uptake and prolonged retention. The molecule is labeled with the radioisotope Lutetium-177 (&sup{177}Lu), which emits beta particles that deliver localized cytotoxic radiation to induce DNA damage and cell death in tumor tissues.
- Other names
- [177Lu]Lu-FAPI-RGDLutetium-177 FAPI-RGDLutetium177 FAPI-RGDLutetium 177 FAPI-RGD177Lu-FAP-RGD
02
Targets
FAP (Fibroblast activation protein alpha)αVβ3 (Integrin αVβ3)ITGAV (Integrin αV)ITGB3 (Integrin beta-3)
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