177Lu-LNC1009

177Lu-LNC1009 is a dual-targeting therapeutic radiopharmaceutical developed by LNC Pharma, a subsidiary of Dongcheng Pharmaceutical Group. It is designed to target both fibroblast activation protein (FAP) and integrin αvβ3, which are frequently overexpressed in the tumor microenvironment and on various malignant cells, respectively. The compound is synthesized using an Evans blue (EB) moiety to enhance albumin binding and extend blood circulation, a FAPI-02 inhibitor for FAP targeting, and a cyclic RGDfK peptide for integrin αvβ3 targeting. Labeled with the beta-emitting radioisotope lutetium-177 (177Lu), the drug delivers targeted ionizing radiation to induce DNA damage and cell death in FAP-positive and integrin αvβ3-positive advanced solid tumors. Preclinical studies have demonstrated high tumor uptake and significant therapeutic efficacy in models of lung and ovarian cancer. The drug received clinical trial approval from China's National Medical Products Administration (NMPA) in late 2025.