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J Nucl Med. 2008; 49 (Supplement 1):95P
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Radiopharmaceutical Chemistry: Radiopharmacy

Radiopharmacy II

A direct procedure for the production of 211At-labeled antibodies using an {epsilon}-lysyl-3-(trimethylstannyl)benzamide immunoconjugate

Sture Lindegren1, Sofia Frost1, Tom Bäck1, Haglund Elin1, Jörgen Elgqvist1 and Holger Jensen2

1 Department of Radiation Physics, Clinical Sciences, Göteborg, Sweden; 2 Department of Nuclear Medicine, Cyclotron and PET Unit, Copenhagen, Denmark

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Objectives: Astatine-211-labeled tumor-specific antibodies have long been considered for the treatment of disseminated cancer. However, the limited availability of the nuclide and the poor efficacy of labeling procedures at clinical amounts of activity present major obstacles to its use. The objective of this study was to evaluate a procedure for direct astatination of antibodies to enable production of clinical levels of activity.

Methods: The monoclonal antibody Herceptin was conjugated with the N-succinimidyl 3-(trimethylstannyl)benzoate (m-MeATE) reagent and the immunoconjugate was then labeled with astatine. Prior to astatination of the conjugated antibody, the nuclide was activated using N-iodosuccinimide. The labeling reaction was evaluated regarding reaction time, volume of reaction solvent, immunoconjugate concentration and applied activity. The quality of the astatinated antibodies was determined by in vitro analysis and biodistribution in nude mice.

Results: The reaction proceeds almost instantaneously and results showed low dependence on reaction volume and immunoconjugate concentration. Radiochemical yields were in the range of 67%-81% and specific radioactivities up to 1 GBq/mg could be achieved. Stability, immunoreactivity and radiochemical purity were equal to or better than the conventional two-step procedure. The tissue distribution in non-tumor-bearing nude mice showed only minor difference in organ uptake compared to the conventional method.

Conclusions: This direct astatination procedure enables high-yield production of astatinated antibodies with high specific activity at the amounts required for clinical applications.





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