212Pb-TCMC-trastuzumab

212Pb-TCMC-trastuzumab is a radioimmunoconjugate composed of the recombinant humanized monoclonal antibody trastuzumab conjugated to the bifunctional chelating agent TCMC (S-2-(4-isothiocyanatobenzyl)-1,4,7,10-tetraaza-1,4,7,10-tetra(2-carbamoylmethyl)cyclododecane), which is then radiolabeled with the alpha-emitting isotope lead-212 (Pb-212). The drug targets human epidermal growth factor receptor type 2 (HER2)-expressing malignancies. Upon binding to HER2 on tumor cells via trastuzumab’s specificity and internalization properties, the radioactive payload delivers localized ionizing radiation that induces cytotoxicity primarily through DNA damage. This approach aims to maximize tumor cell kill while minimizing irradiation of surrounding healthy tissue. It has been investigated in phase I clinical trials for patients with peritoneal carcinomatosis who have failed standard therapies[1][3][5]. The drug was originally developed by AREVA Med (now Orano Med) in collaboration with academic partners[2].

Other names

lead Pb 212 TCMC-trastuzumab