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Bromine-80m Radiotoxicity and the Potential for Estrogen Receptor-directed Therapy with Auger Electrons¹

Ben May Institute [E. R. D., A. H.], Franklin McLean Institute [P. V. H., S. J. G., O. T. D.], and Department of Radiation Oncology [J. L. S.], University of Chicago, Chicago, Illinois 60637; and Argonne National Laboratory [R. C. M., O. T. D.], Argonne, Illinois 60439

While theoretically feasible, estrogen receptor (ER)-directed radiotherapy of hormone-dependent cancers has not been realized because no ER-seeking ligand with an appropriate radiotoxic potential has been identified. Since an appropriate nuclide is a key component we studied the 4.4-h half-life, Auger electron-emitting nuclide bromine-80m. When incorporated into DNA this nuclide was radiotoxic to cells in culture and caused substantial chromosomal damage, while similar concentrations of bromine-80m as bromide or bromoantipyrine were without effect. The mean lethal dose for bromine-80m was 45 atoms per nucleus which is consistent with use in receptor-positive cancers with limited numbers of ER.

¹ These studies were supported by the NIH (CA27476 and HD15513), DOE (contract W-31-109-Eng-38), and by the Julius J. Reingold Fellowship Fund.

² To whom requests for reprints should be addressed, at the Ben May Institute, University of Chicago, 5841 South Maryland Avenue, Chicago, IL 60637.

³ Current address: Medical Division, Brookhaven National Laboratories, Associated Universities, Inc., Upton, Long Island, NY 11973.

⁴ Current address: Department of Medical Physics, University of Wisconsin Medical Center, 1300 University Avenue, Madison, WI 53706.

Received 3/16/88. Revised 7/ 6/88. Accepted 7/15/88.