Astatine antibodies labelled with

Harrison and Royle s experiments109,110 with 211At-labelled anti-Thy 1.1 IgG,OX7 monoclonal antibody appeared more promising. When used for treating Thy 1.1T cell lymphoma in mice, the astatinated antibody was stable in vivo and considerably increased the median survival time. Injection of 80-90 kBq (ca 2.2-2 A fiCi) [211At]astato-OX7 resulted in a complete cure—i.e.survival over 200 days—in 78% of the treated mice. 

Astatine-211 is a promising radionuclide for systemic therapy1 3 due to its decay properties with a half-life of 7.2 hours and an effective emission of one a-particle per decay. However, the weakness of the astatine-protein bond formed after direct astatination1 4 has so far limited its clinical use. To overcome these problems indirect labelling methods have been tried such as the use of ALsuccinimidyl-(trialkylstannyl) benzoate as an intermediate for the astatination of antibodies using conjugation procedures.5 8... 

Zalutsky M R, Garg P K, Friedman F[ S, et al. (1989). Labeling monoclonal antibodies and F(ab )2 fragments with the a-particle-emitting nuclide astatine-211 Preservation of immunoreactivity and in vivo localizing capacity. Proc. Natl. Acad. Sci. USA. 86 7149-7153. 

Wilbur, D. S., Thakar, M. S., Hamlin, D. K. et al. 2009b. Reagents for astatination of biomolecules. 4. Comparison of maleimido-do o-decaborate(2-) and mefa-[211 At]astatobenzoate conjugates for labeling anti-CD45 antibodies with [211 At]astatine. Bioconjugate Chem., 20, 1983-91. 

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