Publications [#65223] of Michael R. Zalutsky

Papers Published

1. Vaidyanathan, G. and Zalutsky, M.R., Targeted therapy using alpha emitters, Phys. Med. Biol. (UK), vol. 41 no. 10 (1996), pp. 1915 - 31 [005]
   (last updated on 2007/04/15)

   Abstract:
   Radionuclides such as ²¹¹At and ²¹²Bi which decay by the emission of α-particles are attractive for certain applications of targeted radiotherapy. The tissue penetration of ²¹²Bi and ²¹¹At α-particles is equivalent to only a few cell diameters, offering the possibility of combining cell-specific targeting with radiation of similar range. Unlike the β-particles emitted by radionuclides such as ¹³¹I and ⁹⁰Y, α-particles are radiation of high linear energy transfer and thus greater biological effectiveness. Several approaches have been explored for targeted radiotherapy with ²¹²Bi- and ²¹¹At-labelled substances including colloids, monoclonal antibodies, metabolic precursors, receptor-avid ligands and other lower molecular weight molecules. An additional agent which exemplifies the promise of α-emitting radiopharmaceuticals is meta-[²¹¹At]astatobenzylguanidine. The toxicity of this compound under single-cell conditions, determined both by [³H]thymidine incorporation and by limiting dilution clonogenic assays, for human neuroblastoma cells is of the order of 1000 times higher than that of meta-[¹³¹I]iodobenzylguanidine. For meta-[²¹¹At]astatobenzylguanidine, the D₀ value was equivalent to only 6-7 ²¹¹At atoms bound per cell. These results suggest that meta-[²¹¹At]astatobenzylguanidine might be valuable for the targeted radiotherapy of micrometastatic neuroblastomas

   Keywords:
   alpha-particle sources;cellular effects of radiation;radiation therapy;radioisotopes;reviews;