177Lu-LNC1008

177Lu-LNC1008 is a novel radioligand therapy (RLT) developed by Yantai Lannacheng Biotechnology, a subsidiary of Dongcheng Pharmaceutical. It consists of the beta-emitting radioisotope Lutetium-177 conjugated to a small molecule ligand that targets Fibroblast Activation Protein (FAP). FAP is highly expressed on cancer-associated fibroblasts (CAFs) within the stroma of over 90% of epithelial solid tumors, including pancreatic, breast, and colorectal cancers, while showing minimal expression in healthy adult tissues. The LNC1008 ligand incorporates an Evans Blue (EB) derivative, which facilitates reversible binding to serum albumin. This modification is designed to extend the drug's circulatory half-life and enhance its accumulation within the tumor microenvironment. Once bound to FAP-expressing cells, the Lutetium-177 delivers localized ionizing radiation, inducing DNA double-strand breaks and subsequent cell death in both the CAFs and adjacent tumor cells via the bystander effect.

Other names

177Lu-EB-FAPI-B1Lutetium (177Lu) LNC1008