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BAY 2701439 (HER2-TTC) is a targeted alpha therapy (TAT) radiopharmaceutical developed by Bayer in collaboration with Lumiphore. It consists of the alpha-emitting radioisotope thorium-227 complexed with a 3,2-hydroxypyridinone (HOPO) chelator, which is conjugated to a monoclonal antibody based on the trastuzumab sequence targeting the human epidermal growth factor receptor 2 (HER2). The mechanism of action relies on the high-energy, short-range alpha particles emitted by thorium-227 to induce potent and selective DNA double-strand breaks in HER2-overexpressing tumor cells, while minimizing damage to adjacent healthy tissue. The agent is designed for the treatment of HER2-positive advanced malignancies, including breast, gastric, and gastro-esophageal cancers, and is currently in Phase 1 clinical development.
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