Drug intelligence / Profile preview

177Lu-FAPI-RGD

Development stage
Phase 1
Lead developer
Peking Union Medical College Hospital
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, 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)

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