[177Lu]Lu-CMT1

[177Lu]Lu-CMT1 is a novel, high-affinity, bicyclic peptide-based radioligand targeting B7-H3 (CD276). Developed by researchers at Stanford University, it targets B7-H3, a transmembrane protein and immune checkpoint molecule overexpressed in approximately 60% of all cancer types. [177Lu]Lu-CMT1 was developed through the systematic optimization of a bicyclic peptide lead structure, incorporating N-terminal modifications, unnatural amino acids, a C-terminal carboxylic acid switch, a PEG3 linker, and a DOTA chelator. Radiolabeled with Lutetium-177, [177Lu]Lu-CMT1 exhibits high target affinity (KD of 22.5 nM on B7-H3-expressing T-47D cells), favorable hydrophilicity, and rapid clearance from healthy organs in preclinical models, holding promise for targeted radiopharmaceutical therapy of multiple cancer types.

Other names

177Lu-CMT1Lu-CMT1Lu-CMT-1Lu-CMT 1