actinium-225-DOTA-trastuzumab

Actinium-225-DOTA-trastuzumab is an experimental targeted alpha-particle therapy (TAT) consisting of the HER2-targeting monoclonal antibody trastuzumab conjugated via a DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) chelator to the alpha-emitting radioisotope actinium-225. It is designed to treat HER2-positive malignancies, including breast cancer and associated brain metastases, by delivering high-linear energy transfer (LET) radiation directly to cancer cells expressing the human epidermal growth factor receptor 2 (HER2/neu). The alpha particles emitted by actinium-225 have a short tissue range of approximately 50–80 μm, which allows for potent cytotoxic effects on targeted cells through double-strand DNA breaks while minimizing damage to surrounding healthy tissue. This radiopharmaceutical is being investigated in preclinical studies as a potential treatment for patients who have progressed on standard HER2-targeted therapies and as part of a theranostic strategy.

Other names

Actinium-225-labeled trastuzumabActinium225-labeled trastuzumabActinium 225-labeled trastuzumab225Ac-trastuzumab