In vitro testing of the leukaemia monoclonal antibody WM-53 labeled with alpha and beta emitting radioisotopes

We report the preparation and testing of a new alpha emitting radio-immunoconjugate (RIC) against acute myeloid leukaemia (AML) using CD33 positive monoclonal antibody WM-53 (specific for HL-60 cell line). Using cyclic anhydride of diethylenetriaminepentacetic acid (cDTPAa) as chelator, antibody was labeled with 213 Bi (alpha), 149 Tb (alpha), 153 Sm (beta) and 152 Tb (positron). In vitro testing showed high labeling efficiency (90–95%) and stability (11–19% leaching) with immunoreactivity virtually the same before and after labeling. DNA synthesis data and MTS cell survival were compared for all RICs. Only the alpha emitter was found to be capable of inhibiting DNA synthesis and had selective cell kill with activity as low as 2–3 μCi. The high stability and outstanding cytotoxicity of the 213 Bi conjugate provides the basis for targeted alpha therapy for the control of metastatic and disseminated cancer such as AML.