68Ga/177Lu-labeled nectin4-targeted covalent bicyclic peptide: a novel nectin-4-targeted radioligands for theranostic of urothelial carcinoma - PubMed
4 days ago
- #Nectin-4
- #Urothelial Carcinoma
- #Theranostic
- Nectin-4 is overexpressed in urothelial carcinoma (UC) and is a promising target for theranostic applications.
- FDA-approved enfortumab vedotin has shown efficacy in UC treatment.
- 68Ga/177Lu-FZ-NRs, a novel Nectin-4-targeted radioligand, was developed for PET/CT imaging and radiotherapy.
- In vitro studies showed high radiochemical purity, stability, and strong Nectin-4 affinity for 68Ga/177Lu-FZ-NRs.
- MicroPET/CT imaging confirmed strong tumor enrichment and low off-target binding for 68Ga-FZ-NRs.
- Clinical translation demonstrated precise lesion localization in UC patients, matching 18F-FDG and high Nectin-4 expression areas.
- 177Lu-FZ-NRs showed higher tumor uptake and retention, enhancing therapeutic effects with strong tumor growth inhibition and low toxicity.
- The study provides new molecular imaging tools for Nectin-4 assessment and establishes a foundation for UC-targeted radiotherapy.