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Sodium borocaptate is a boron-containing small molecule developed as a therapeutic agent for use in Boron Neutron Capture Therapy (BNCT), primarily for the treatment of malignant brain tumors such as glioblastoma multiforme. After intravenous administration, it preferentially accumulates in tumor cells. Upon exposure to neutron irradiation, the ^10B isotope within sodium borocaptate absorbs neutrons and undergoes nuclear fission to release high-energy alpha particles and lithium nuclei. This process causes highly localized cytotoxicity within tumor cells while sparing surrounding normal tissue due to the short path length of emitted radiation. Sodium borocaptate was originally developed by Shionogi and has been evaluated in phase I clinical trials for glioma, thyroid cancer, head and neck cancer, and liver metastases from colorectal cancer[3][4][6]. Its development for glioma was discontinued.
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