BSH

BSH (CAS No. 144885-51-8) is the first clinically used boron delivery agent for Boron Neutron Capture Therapy (BNCT), a targeted cancer treatment that relies on BSH’s ability to selectively deliver boron-10 (^10B) to tumor tissues via intravenous or arterial injection. When exposed to low-energy thermal neutrons, ^10B undergoes nuclear fission, releasing high-energy alpha particles and lithium-7 nuclei that precisely destroy tumor cell DNA while sparing healthy tissue. Animal studies confirm BSH achieves a high tumor-to-blood boron ratio, and clinical data show its tumor accumulation depends on blood-brain barrier (BBB) disruption—only regions with a compromised BBB effectively take up BSH. At medium doses (15–100 mg/kg), BSH reaches therapeutic boron concentrations in tumors with a favorable tumor-to-normal brain ratio, while higher doses increase nephrotoxicity risk without added benefit. Although BSH delivers higher boron levels to tumors than to normal tissues, its effectiveness is limited by variable uptake due to uneven BBB disruption. Overall, BSH has been foundational in BNCT, demonstrating targeted tumor delivery and paving the way for improved boron agents.

References：

[1] Barth RF, Gupta N, Kawabata S. Evaluation of sodium borocaptate (BSH) and boronophenylalanine (BPA) as boron delivery agents for neutron capture therapy (NCT) of cancer: an update and a guide for the future clinical evaluation of new boron delivery agents for NCT. Cancer Commun (Lond). 2024 Aug;44(8):893-909. doi: 10.1002/cac2.12582. Epub 2024 Jul 8. PMID: 38973634; PMCID: PMC11337926.