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177Lu-FZ-NR-1 is a nectin-4-targeted radiopharmaceutical consisting of a bicyclic peptide (FZ-NR-1) labeled with the beta-emitting radionuclide lutetium-177. It is designed for the targeted radiotherapy of tumors overexpressing Nectin-4, such as urothelial carcinoma and triple-negative breast cancer. In preclinical studies, it serves as a non-covalent reference compound compared against newer covalent-binding radioligands (covalent 177Lu-FZ-NRs) developed using a SuFEx-bio-orthogonal strategy. The drug works by binding to Nectin-4 on the surface of cancer cells, allowing for the localized delivery of ionizing radiation to induce DNA damage and cell death. It was developed by researchers at Fudan University Shanghai Cancer Center.
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