211At-lintuzumab-bisB10

211At-lintuzumab-bisB10 is a preclinical targeted alpha therapy (TAT) radioconjugate consisting of the humanized anti-CD33 monoclonal antibody lintuzumab conjugated to a novel bis-closo-decaborate(4-) (bisB10) reagent (bisB10-PEG2-NCS) and radiolabeled with the alpha-emitting isotope astatine-211 (211At). Developed by the University of Washington and the Fred Hutchinson Cancer Center, this agent is designed to target CD33-expressing myeloid leukemia cells, such as those in acute myeloid leukemia (AML). The bisB10 reagent features dual nucleophilic sites that provide intramolecular stabilization of 211At, significantly reducing 211At-mediated antibody dimer formation and enhancing stability against in vivo deastatination. This results in higher tumor uptake and lower accumulation in deastatination-sensitive organs like the stomach and large intestine compared to traditional B10-NCS-conjugated formulations, potentially improving radiochemical purity and reducing off-target toxicities.

Other names

211At-bisB10-lintuzumab211At-labeled bisB10-lintuzumabastatine-211 lintuzumab-bisB10astatine211 lintuzumab-bisB10astatine 211 lintuzumab-bisB10