TARGETED ALPHA PARTICLE THERAPY USING ACTINIUM-225 CONJUGATES

摘要

The present invention provides functionalized chelants and a method of treating cancerous cells with alpha particles comprising the step of administering a pharmacologically effective dose of an 225Ac conjugate comprising a functionalized chelant R is independently CHQCO2X; Q is independently hydrogen; C1-C4 alkyl or (C1-C2 alkyl) phenyl; X is independently hydrogen; benzyl or C1-C4 alkyl; Z1 is (CH2)nY where n is 1-10 and Y is an electrophilic or nucleophilic moiety and Z2 is R; or, alternatively, Z1 is hydrogen and Z2 is a peptide linker composed of 1-10 amino acids; said Y or said peptide linker covalently attached to an antibod y or fragment thereof, or other biologic molecule; or a pharmaceutically acceptable salt thereof, complexed with 225Ac. These biologic molecule binds to cancerous cells and 225Ac or its daughters emit alpha particles into said cancerous cells effecting treatment.