Synthesis of Auger Electron-Emitting Radiopharmaceuticals

Author: Hanson, R.N.

Source: Current Pharmaceutical Design, Volume 6, Number 14, 1 September 2000 , pp. 1457-1468(12)

Publisher: Bentham Science Publishers

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Abstract:

Targeted radiotherapy using Auger electron-emitting pharmaceuticals offers both advantages and challenges compared to alternative alpha - or beta -emitting agents. The low energy Auger electrons deposit their energy within the target cell thereby minimizing collateral damage. To achieve this effect, however, the radiopharmaceutical must incorporate the appropriate radionuclide, be efficiently synthesized, and once administered, be distributed selectively to its biological target. This review covers the synthesis of agents which have prepared over the past decade either as Auger electron-emitting radiopharmaceuticals or which have the potential as such. While not an exhaustive review, the major classes of agents, such as hormone receptor ligands, nucleoside analogs and intercalating agents are described.

Keywords: Synthesis; Auger Electron emitting Radiopharmaceuticals; Targeted radiotherapy; Hormone receptor ligands; Nucleoside analogs; Intercalating agents; Chromium 51; Gallium 67; Bromine 77, 80m; Indium 111; Iodine 123, 125; Platinum 193m; Thallium 201; Hormone receptor ligands; Nuclear Receptor Binding; DNA directed agents; Estrogen receptor ligands; Radiodiagnostic PET and SPECT; Flutamide; Anandron; Bicalutamide; Iodo bicalutamide; DNA directed agents; Radioiodinated oligonucleotides