111In-NLS-nimotuzumab

111In-NLS-nimotuzumab is an experimental Auger electron-emitting radioimmunotherapeutic agent developed by the University of Toronto in collaboration with YM Biosciences. It consists of nimotuzumab, a humanized monoclonal antibody targeting the epidermal growth factor receptor (EGFR), conjugated to the radionuclide Indium-111 (111In) via a benzyl-DTPA (bn-DTPA) chelator and modified with nuclear localization sequence (NLS) peptides. The NLS peptides facilitate the translocation of the radioimmunoconjugate into the cell nucleus after EGFR-mediated internalization. Once inside the nucleus, the short-range Auger electrons emitted by Indium-111 cause lethal double-strand DNA breaks. This targeted radiotherapeutic approach is designed to treat EGFR-overexpressing and trastuzumab-resistant breast cancers, including triple-negative breast cancer, while minimizing toxicity to normal tissues with lower EGFR expression.

Other names

111In-Bn-DTPA-nimotuzumab with NLS peptide modification111In-NLS-Bn-DTPA-nimotuzumab111In-NLS-Nmab111In-labeled nimotuzumab modified with nuclear localization sequences