ABSTRACT
This chapter focuses on advances in the chemistry for monoclonal antibodies (MoAb) radiolabeling by use of chelators specifically synthesized for complexation of the positron emitter Gallium (Ga), the ß-emitter Y, and the α-particle sources Bi, and Pb. Therapeutic use of MoAb radiolabeled with cytocidal radionuclides is proving to be advantageous in the treatment of leukemia and lymphoma. In principle, ß+ emitting radionuclides could be used for therapeutic applications. Two radiochemical approaches to the radiolabeling of immunoproteins are employed. Direct chemical reaction is often used with radionuclides of iodine or, to a lesser extent, technetium and rhenium, that easily form relatively stable chemical bonds with protein amino acid residues. X-ray crystallographic studies of the neutral complex demonstrated full N3O3 coordination and suggested that NOTA might be useful for MoAb-mediated delivery of Ga to tumor cells. Clinical studies using Y-labeled MoAb anti-Tac have established the potential of Y-chelate-labeled antibodies as anti-tumor agents.
