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JR11-TCO is a somatostatin receptor subtype 2 (SSTR2) antagonist peptide (JR11) covalently modified with a trans-cyclooctene (TCO) group and a DOTA chelator. It is developed for use in a pretargeted radionuclide therapy strategy for neuroendocrine tumors (NETs). In this approach, JR11-TCO is administered first to target and bind SSTR2-expressing tumor cells. Subsequently, a radiolabeled tetrazine (Tz) molecule (such as [111In]In-tetrazine) is administered, which rapidly and selectively conjugates with the prelocalized JR11-TCO via an in vivo bioorthogonal inverse electron-demand Diels-Alder (IEDDA) click chemistry reaction. This pretargeting strategy aims to deliver high doses of therapeutic radiation to the tumor while minimizing systemic exposure and healthy organ accumulation.
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