NEW GADOLINIUM-BORON COMPOUNDS FOR NEUTRON CAPTURE THERAPY

NEUTRON CAPTURE THERAPY IS A VERY PROMISING THERAPY FOR CERTAIN TUMORS, SUCH AS GLIOMAS AND MELANOMAS. SEVERAL NUCLEI HAVE HIGH CROSS SECTIONS FOR THERMAL NEUTRONS, OF WHICH BORON-10 ((10)B) AND GADOLINIUM-157 ((157)GD) HAVE BEEN SHOWN TO BE VERY PROMISING. (10)B HAS A HIGH CROSS SECTION FOR THERMAL NEUTRONS AND A VERY VERSATILE CHEMISTRY. (157)GD HAS THE HIGHEST CROSS SECTION FOR THERMAL NEUTRONS AND, BEING PARAMAGNETIC, IS GOOD FOR MAGNETIC RESONANCE IMAGING. A COMBINATION OF THESE TWO NUCLEI IN A SINGLE ENTITY SHOULD PROVIDE A SINGLE, MORE CONVENIENT WAY TO DIAGNOSE AND TREAT TUMORS. PHASE I RESEARCH FOCUSES ON THE SYNTHESIS OF A MOLECULE CONTAINING BOTH (10)B AND (157)GD AND ON EVALUATING ITS STABILITY, TOXICITY (LD50), AND IN-VITRO EFFICACY. PHASE II RESEARCH WILL BE CONCERNED WITH THE EVALUATION OF IN-VIVO EFFICACY, STRUCTURE-ACTIVITY RELATIONSHIP STUDIES TO OPTIMIZE EFFICACY AND DETERMINE THE PHARMACOKINETICS, TISSUE DISTRIBUTION, AND TOXICITY (SAFETY) OF LEAD COMPOUND(S).