RADIOIMMUNOTHERAPY WITH ALPHA-EMITTING NUCLIDES

This review discusses the application of alpha particle-emitting radio nuclides in targeted radioimmunotherapy. It will outline the productio n and chemistry of astatine-211 bismuth-212, lead-212, actinium-225, b ismuth-213, fermium-255, radium-223 and terbium-149, which at present are the most promising alpha-emitting isotopes available for human cli nical use. The selective cytotoxicity offered by alpha particle-emitti ng radioimmunoconstructs is due to the high linear energy transfer and short particle path length of these radionuclides. Based upon the pha rmacokinetics of alpha particle-emitting radioimmunoconstructs, both s tochastic and conventional dosimetric methodology is discussed, as is the preclinical and initial clinical use of these radionuclides conjug ated to monoclonal antibodies for the treatment of human neoplasia.