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177Lu-HGC254
- Development stage
- Unknown
- Lead developer
- West China Hospital of Sichuan University
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals
- Administration
- Intravenous
01
Overview
177Lu-HGC254 is an investigational radioligand therapy consisting of the beta-emitting radionuclide lutetium-177 (177Lu) conjugated to HGC254, a targeting ligand that binds to fibroblast activation protein (FAP). FAP is highly expressed on cancer-associated fibroblasts (CAFs) in the tumor stroma of various advanced solid tumors, including pancreatic, gastric, and colorectal cancers, while showing low expression in normal tissues. Upon binding to FAP, 177Lu-HGC254 delivers targeted radiation directly to the tumor microenvironment, inducing DNA damage and cell death in both FAP-expressing cells and neighboring tumor cells via the bystander effect. It is being evaluated in early-phase clinical trials for the treatment of FAP-positive advanced solid tumors.
02
Targets
DNAFAP (Fibroblast activation protein alpha)
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