Development of a new tumor seeking compound for neutron capture therapy

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Three types of boronated manganese metalloporphyrin (STA-BX900, STA-BX909, STABX910) for neutron capture therapy has been developed.Results1.In vivo boron concentration study revealed highest tumor boron concentration in STA-BX909 followed by STA-BX900 and STA-BX910 24 hours after intravenous injection of 0.05mmol/kg dose. This tendency was correlated with the liver boron concentration. From this result, STA-BX909 was chosen for further radiobiological study.2.In vitro boron concentration analysis : In the cultured 9L gliosarcoma cell line, the boron concentration was stable with BSH added condition medium even after 24 hours. STA-BX909 showed increase in boron concentration as a function of time. In BSH,the intracellular boron concentration may be dependent on the medium boron concentration. STA-BX909 progressively accumulated in tumor cells and the increase of boron concentration indicated an active uptake mechanism.3.Neutron irradiation revealed also stronger biological effect with STA-BX909 than BSH and least with neutron irradiation without boron compound.As conclusions, boronated metalloporphyrin is a potential boron carrier for boron neutron capture therpay for malignant brain tumors. Further basic research is warranted to develop a clinically applicable drug.