Specific Cytotoxicity of Targeted 177Lu and 212Pb-Based Radiopharmaceuticals

Two radiopharmaceutical preparations were developed on the basis of artificial targeted polypeptide ZHER2 specific to HER2/neu tumor marker and radionuclides 177 Lu (ZHER2-HSA-chelator- 177 Lu) or 212 Pb (ZHER2-HSA-chelator- 212 Pb). The objective was to evaluate in vitro the cytotoxic activity of t...

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Bibliographic Details
Published in:Bulletin of experimental biology and medicine 2021-09, Vol.171 (5), p.627-632
Main Authors: Pankratov, A. A., Nemtsova, E. R., Plyutinskaya, A. D., Vorontsova, M. S., Chuvilin, D. Yu, Egorova, B. V., Kokov, K. V., Deev, S. M., Lebedenko, E. N., Proshkina, G. M., Shul’ga, A. A., Golovachenko, V. A., Shegai, P.V., Kaprin, A. D.
Format: Article
Language:English
Subjects:
Biomedical and Life Sciences
Biomedicine
Breast cancer
Cell Biology
Cytotoxicity
ErbB-2 protein
Internal Medicine
Laboratory Medicine
Pathology
Pharmaceuticals
Radioisotopes
Salts
Tumor cell lines
Tumor markers
Tumors
Xenografts
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Summary:Two radiopharmaceutical preparations were developed on the basis of artificial targeted polypeptide ZHER2 specific to HER2/neu tumor marker and radionuclides 177 Lu (ZHER2-HSA-chelator- 177 Lu) or 212 Pb (ZHER2-HSA-chelator- 212 Pb). 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.
ISSN:0007-4888
1573-8221
DOI:10.1007/s10517-021-05283-4