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Comparative Serum Stability of Radiochelates for Antibody Radiopharmaceuticals

Division of Nuclear Medicine, University of California Davis Medical Center, Sacramento
Department of Chemistry, University of California, Davis
Department of Pathology, University of Southern California, Los Angeles, California
Los Alamos National Laboratory, Los Alamos, New Mexico

Correspondence: For reprints contact: Sally J. DeNardo, MD, Div. of Nuclear Medicine, 4301 X St., FOLB II-E, University of California Davis Medical Center, Sacramento, CA 95817.

ABSTRACT

Serum incubation of monoclonal antibodies chelate labeled by DTPA, benzyl-EDTA and benzyl-TETA with ¹¹¹In, ⁵⁷Co, and ⁶⁷Cu demonstrated marked differences in their stability. In serum, ¹¹¹In-benzyl-EDTA-antibody was more stable than ¹¹¹In-DTPA-antibody. Cobalt-57 or ⁶⁷Cu chelated antibody were less stable than either ¹¹¹In chelated antibody; ⁶⁷Cu was only firmly attached to the antibody as ⁶⁷Cu-benzyl-TETA-antibody. The relative stability of the radiometal chelated antibodies was paralleled by the relative stability in serum of the radiometal chelates themselves. These in vitro studies suggest that in vivo behavior of metal chelates exposed to a complex protein environment cannot be predicted by classical equilibrium constants.

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