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213Bi-lintuzumab is a first-generation targeted alpha-particle therapy (TAT) consisting of the humanized anti-CD33 monoclonal antibody, lintuzumab (HuM195), conjugated to the alpha-emitting radioisotope Bismuth-213 (213Bi). It is primarily investigated for the treatment of acute myeloid leukemia (AML), where it targets the CD33 antigen expressed on the surface of myeloid leukemic cells. Upon binding, the conjugate delivers high-energy alpha particles directly to the tumor cells, inducing lethal double-strand DNA breaks. Because alpha particles have a very short path length (50–80 μm), they provide potent cytotoxicity to targeted cells while sparing surrounding healthy tissue. Development of this specific construct was largely led by researchers at Memorial Sloan Kettering Cancer Center (MSKCC). However, the clinical utility of 213Bi-lintuzumab has been constrained by the short 46-minute half-life of the 213Bi isotope, which necessitates an onsite generator for radiolabeling and rapid administration.
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