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Comparative Tissue Distribution in Mice of the -Emitter ²¹¹At and ¹³¹I as Labels of a Monoclonal Antibody and F(ab')₂ Fragment¹

Departments of Radiology [P. K. G., C. L. H., M. R. Z.] and Pathology [M. R. Z.], Duke University Medical Center, Durham, North Carolina 27710

Because it decays by the emission of short-range, high-energy -particles, the radiohalogen ²¹¹At might be a particularly useful nuclide for some types of radioimmunotherapy. However, no suitable -emitting nuclide of astatine exists whch would permit either imaging prior to therapy to obtain radiation dosimetry estimates or performing experiments in paired-label format. Since iodine is the halogen above astatine in the periodic table, we investigated whether the in vivo distribution of ¹³¹I could be used to mimic the biodistribution of ²¹¹At. In this study, the N-succinimidyl 3-(trialkylstannyl)benzoate method was used to label C110 IgG, an antibody directed against carcinoembryonic antigen, and its (Fab')₂ fragment with ²¹¹At and ¹³¹I. Paired-label experiments were performed in normal mice comparing the tissue distribution of ²¹¹At-versus ¹³¹I-labeled C110 IgG and F(ab')₂ as well as [²¹¹At]astatide versus [¹³¹I]iodide and m-[²¹¹At]astatobenzoic acid versus m-[¹³¹I]iodobenzoic acid, potential catabolites of proteins radiohalogenated via the N-succinimidyl 3-(trialkylstannyl)benzoate method. With the exception of thyroid, retention of astatide in tissues was higher than that of iodide; and, with the halobenzoic acids, uptake of ²¹¹At was higher than ¹³¹I in thyroid, stomach, and spleen. Use of the N-succinimidyl 3-(trialkylstannyl)benzoate method to label C110 IgG with ²¹¹At and ¹³¹I resulted in similar distributions of the two nuclides. In contrast, loss of ²¹¹At from the F(ab')₂ fragment was considerably more rapid than ¹³¹I, suggesting that different astatination methods may be required for use with F(ab')₂ fragments.

¹ Supported by National Cancer Institute Grants CA 42324, NS 20023, and CA 14236 and by Grant DE-FG05-89ER60789 from the Department of Energy.

² To whom requests for reprints should be addressed, at Department of Radiology, Box 3808, Duke University Medical Center, Durham, NC 27710.

Received 11/27/89. Revised 2/14/90.

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