Two radiopharmaceutical preparations were developed on the basis of artificial targeted polypeptide ZHER2 specific to HER2/neu tumor marker and radionuclides 177Lu (ZHER2-HSA-chelator-177Lu) or 212Pb (ZHER2-HSA-chelator-212Pb). The objective was to evaluate in vitro the cytotoxic activity of the targeted radiopharmaceuticals using two cultured human breast cancer cell lines with different expression of HER2/neu: SK-BR3 (high expression of HER2/neu) and MCF-7 (low expression of HER2/neu). It was shown that the cytotoxic effect of both preparations was significantly higher against the SK-BR-3 cells. The cytotoxicity correlated with the incubation period (it was higher after 72 h than after 24 h) and was significantly more pronounced in comparison with activity of radionuclide salts without a specific ligand. In vivo preclinical study of these pharmaceuticals seems to be very promising in animals with xenografted tumors showing high expression of HER2/neu marker.
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Translated from Byulleten’ Eksperimental’noi Biologii i Meditsiny, Vol. 171, No. 5, pp. 601-607, May, 2021
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Pankratov, A.A., Nemtsova, E.R., Plyutinskaya, A.D. et al. Specific Cytotoxicity of Targeted 177Lu and 212Pb-Based Radiopharmaceuticals. Bull Exp Biol Med 171, 627–632 (2021). https://doi.org/10.1007/s10517-021-05283-4
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DOI: https://doi.org/10.1007/s10517-021-05283-4