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67Cu-Sar-NTSR is an investigational, targeted radiotherapeutic (radioligand therapy) consisting of the beta-emitting radioisotope copper-67 (67Cu) chelated by a sarcophagine (Sar) cage moiety and conjugated to a neurotensin receptor 1 (NTSR1) targeting ligand. Developed by the University of North Carolina at Chapel Hill and licensed to Accunovo Biotechnologies, 67Cu-Sar-NTSR is designed to target NTSR1-expressing tumors, such as pancreatic ductal adenocarcinoma (PDAC) and prostate cancer (particularly PSMA-negative or neuroendocrine-transdifferentiated prostate cancer). The sarcophagine chelator provides high stability for the copper radiometal, preventing premature release and off-target toxicity. Upon binding to NTSR1 on cancer cells, the agent is internalized, and the beta emission from 67Cu induces DNA double-strand breaks, leading to tumor cell death. It is studied as a theranostic pair alongside its diagnostic counterpart, 64Cu-Sar-NTSR.
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