BNCT – Drugs for Boron Neutron Capture Therapy

Boron Neutron Capture Therapy (BNCT) is an experimental, binary radiotherapy which is currently being used for treatment of patients with malignant glioma or melanoma in the USA, Japan and Europe. In BNCT a ¹⁰B containing compound is administered to the patient, in whom it accumulates preferentially into the neoplastic tissue. The tumor is then irradiated with low-energy neutrons produced by a nuclear reactor. In the ensuing neutron capture reaction ¹⁰B absorbs neutrons and self-destructs releasing powerful but very short-range alfa radiation and recoil lithium in the tumor. ¹⁰B boron carriers in clinical use are disodium mercaptoundecahydro-closo-dodecaborate (Na₂H₁₁¹⁰B₁₂SH, sodium borocaptate, sodium mercaptododecaborate, BSH) and a boronated aromatic amino acid derivative, L-4-dihydroxyboryl phenylalanine ((HO)₂¹⁰B-C₆H₄-CH(NH₂)CO₂H, 4-borono-L-phenylalanine, L-BPA).

Both of the above mentioned drugs, BSH and L-BPA, are beside Japan and USA continually tested with good results in the states of EU (Holland, Germany, UK, Sweden Finland).  Katchem Ltd. developed the production technology for both drugs. This production of mentioned very expensive and, as regard to work, sophisticated products demands high-qualified workers and, such workers are the employees of our firm. Our products are after analysis (HPLC, ¹H, ¹³C ,¹⁰B NMR and IR spectra) the same quality as the drugs of word prestigious firms. The standard purity of the product is now guaranteed as >99%. Know-how of the synthesis has been handed over to a medium-sized pharmaceutical plant Interpharma Praha, which produces BPA by GMP protocol. BSH production by GMP is discussed.

The competent estimation indicates the rate of malignant brain tumors 60 for one million of inhabitants per year. After Japanese sources, combined treatment of glioblastoma inclusive of surgery intervention, radiation, stereotactic surgery intervention, interstitial therapy and chemotherapy leads to 60 week survival by 1 per cent of patients only. After undergoing BNCT treatment survive 58 per cent of patients 5 years and almost 30 per cent more than 10 years. As regard to patients suffering from skin melanoma, i.e. candidates for L-BPA application, their number is several time higher. 

¹⁰B enriched precursors for BPA, BSH and other borane and carborane derivatives

Katchem team is able to prepare for our partners ¹⁰B enriched borane and carborane derivatives (¹⁰B enrichment >99.5%) as :
sodium borohydride , Na¹⁰BH₄,
triethylamineborane, ¹⁰BH₃.(CH₃CH₂)₃N,
dodecahydrododecaborate dianion ,        ¹⁰B₁₂H₁₂^2-,
decahydrodecaborate dianion with different cations,
decaborane(14) ¹⁰B₁₀H₁₄,
o-carborane C₂¹⁰B₁₀H₁₂
etc.

Many other ¹⁰B enriched compounds could be synthesized by our company after negotiation.

Contact person:

Otomar Kříž, Ph.D.,  Phone: +420-721 334 399,   e-mail: okriz@katchem.cz