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177Lu-FAP-VG11 is an investigational peptide-based radioligand therapy (RLT) developed by VitsGen Therapeutics. It consists of a novel targeting ligand directed against fibroblast activation protein (FAP) chelated with the beta-emitting radioisotope lutetium-177 (177Lu). FAP is highly overexpressed on cancer-associated fibroblasts (CAFs) within the tumor microenvironment of various epithelial malignancies, making it an attractive target for selective radiopharmaceutical delivery. Upon binding to FAP-positive cells, 177Lu-FAP-VG11 is internalized, delivering localized cytotoxic beta radiation that induces DNA damage and cell death in both tumor cells and the supporting stroma. The drug is being developed for the treatment of FAP-positive advanced malignant solid tumors, including pancreatic ductal adenocarcinoma, non-small cell lung cancer (NSCLC), breast cancer subtypes, soft tissue sarcoma, esophageal cancer, cholangiocarcinoma, and urothelial carcinoma of the bladder. It has entered Phase 1 clinical development following IND acceptance by the NMPA CDE and the initiation of an investigator-initiated trial (IIT) in China.
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