177Lu-DOTA-αLAG-3

177Lu-DOTA-αLAG-3 is a novel, preclinical-stage targeted radionuclide therapy (TRT) consisting of the anti-LAG-3 monoclonal antibody relatlimab conjugated to the chelator DOTA and radiolabeled with the beta-emitting radioisotope lutetium-177 (177Lu). Developed by researchers at Tongji University and Shanghai Pulmonary Hospital, this radiopharmaceutical specifically targets Lymphocyte Activation Gene 3 (LAG-3), an inhibitory immune checkpoint receptor highly expressed on exhausted T cells. By delivering localized beta radiation directly to LAG-3-expressing cells in the tumor microenvironment, 177Lu-DOTA-αLAG-3 induces tumor cell necrosis and apoptosis, reduces regulatory T cell (Treg) infiltration, and enhances CD3+ and CD8+ T-cell infiltration. Preclinical studies in lung cancer models demonstrate that 177Lu-DOTA-αLAG-3 significantly inhibits tumor growth, particularly when combined with anti-PD-L1 immunotherapy, suggesting its potential to remodel the tumor immune microenvironment and overcome resistance to immune checkpoint blockades.

Other names

177Lu-DOTA-aLAG-3177Lu-DOTA-relatlimab¹⁷⁷Lu-DOTA-αLAG-3