Evaluation of a Novel Boron-Containing α-d-Mannopyranoside for BNCT

摘要: Boron neutron capture therapy (BNCT) is a unique anticancer technology that has demonstrated its efficacy in numerous phase I/II clinical trials with boronophenylalanine (BPA) and sodium borocaptate (BSH) used as 10B delivery agents. However, continuous drug administration at high concentrations needed to maintain sufficient concentration within tumors. To address the issue of accumulation retention tumor tissue, we developed MMT1242, novel boron-containing α-d-mannopyranoside. We evaluated uptake, intracellular distribution, MMT1242 cultured cells analyzed biodistribution, tumor-to-normal tissue ratio toxicity vivo. Fluorescence imaging using nitrobenzoxadiazole (NBD)-labeled inductively coupled mass spectrometry (ICP-MS) were performed. The effectiveness BNCT was assessed animal irradiation studies Kyoto University Research Reactor. showed uptake broad distribution vitro, longer compared BSH BPA, adequate low A study subcutaneous murine model revealed significant inhibiting effect if injected 24 h before irradiation. therefore report 10B-MMT1242 candidate for further studies.