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177Lu-FZ-NRs
- Development stage
- Preclinical
- Lead developer
- Fudan University Shanghai Cancer Center
- Modality
- Cyclic Peptides → Modified Peptides → Peptides, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
177Lu-FZ-NRs is a novel nectin-4-targeted radiopharmaceutical consisting of a covalent bicyclic peptide labeled with the beta-emitting radionuclide lutetium-177. Developed by researchers at Fudan University Shanghai Cancer Center, it utilizes a sulfur(VI) fluoride exchange (SuFEx) bio-orthogonal strategy to achieve covalent binding to its target, Nectin-4, which is highly expressed in urothelial carcinoma. This covalent mechanism significantly enhances tumor enrichment and retention compared to traditional non-covalent radioligands, leading to potent inhibition of tumor growth with minimal off-target toxicity. It is designed as the therapeutic component of a theranostic pair, with 68Ga-FZ-NRs serving as the companion PET imaging agent for patient selection and monitoring.
- Other names
- 177Lu-labeled nectin-4-targeted covalent bicyclic peptide177Lu-FZ-NR
02
Targets
PVRL4 (Nectin cell adhesion molecule 4)
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