Boron neutron capture therapeutics

Sodium borate was used to treat nearly a dozen patients with BNCT through a collaboration between Massachusetts General Hospital and Brookhaven National Laboratory.

[6][7] Seeking to improve selectivity through chemical modification, studies were performed to correlate lipid solubility with penetration of the blood-brain barrier in mice.

Based on this data, boron-10 enriched samples of p-carboxyphenylboronic acid (PCPB) and sodium decahydrodecaborate (Na2B10H10) were selected for BNCT at the Massachusetts Institute of Technology research reactor.

[13] PCPB and Na2B10H10 had been selected for their promising tumor:normal tissue differentials; however, the concentration of boron-10 in patients’ blood was not considered as significant a concern until after these results.

[1] Building on the dodecaborane anion ([B12H12]2-) discovered in part by M. Frederick Hawthorne, Earl Muetterties et al. developed the monosubstituted derivative sodium borocaptate (BSH, Na2B12H11SH).

Using BSH synthesized by the Shionogi pharmaceutical company, BNCT was used to treat over 200 patients by Hiroshi Hatanaka, Yoshinobu Nakagawa, and their colleagues.

[19][3][20] First synthesized in 1958 by Snyder et al., boronophenylalanine (BPA) and its more water-soluble fructose complex (BPA-F) were not initially acknowledged as potential BNCT therapeutics.

[2] Third-generation boron delivery agents are marked by inclusion of a specific chemical tumor-targeting moiety, often borrowed from those established in chemotherapy, linked to a boron-carrying compound.

[24] Examples of compounds derivativized for BNCT include "peptides, proteins, antibodies, nucleosides, sugars, porphyrins, liposomes and nanoparticles.