Radioimmunotheranostic pair based on the anti-HER2 monoclonal antibody
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2021
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Pharmaceutics
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Resumo
The oncogene HER2 is an important molecular target in oncology because it is associated
with aggressive disease and the worst prognosis. The development of non-invasive imaging
techniques and target therapies using monoclonal antibodies is a rapidly developing field. Thus,
this work proposes the study of the radioimmunotheranostic pair, [111In]In-DTPA-trastuzumab and
[177Lu]Lu-DOTA-trastuzumab, evaluating the influence of the chelating agents and radionuclides on
the biological properties of the radioimmunoconjugates (RICs). The trastuzumab was immunoconjugated
with the chelators DTPA and DOTA and radiolabeled with [111In]InCl3 and [177Lu]LuCl3,
respectively. The stability of the RICs was evaluated in serum, and the immunoreactive and internalization
fractions were determined in SK-BR-3 breast cancer cells. The in vivo pharmacokinetics and
dosimetry quantification and the ex vivo biodistribution were performed in normal and SK-BR-3
tumor-bearing mice. The data showed that there was no influence of the chelating agents and radionuclides
on the immunoreactive and internalization fractions of RICs. In contrast, they influenced
the stability of RICs in serum, as well as the pharmacokinetics, dosimetry and biodistribution profiles.
Therefore, the results showed that the nature of the chelating agent and radionuclide could influence
the biological properties of the radioimmunotheranostic pair.
Como referenciar
MIRANDA, ANA C.C.; SANTOS, SOFIA N. dos; FUSCALDI, LEONARDO L.; BALIEIRO, LUIZA M.; BELLINI, MARIA H.; GUIMARAES, MARIA I.C.C.; ARAUJO, ELAINE B. de. Radioimmunotheranostic pair based on the anti-HER2 monoclonal antibody: influence of chelating agents and radionuclides on biological properties. Pharmaceutics, v. 13, n. 7, p. 1-16, 2021. DOI: 10.3390/pharmaceutics13070971. Disponível em: http://repositorio.ipen.br/handle/123456789/32304. Acesso em: 24 Apr 2024.
Esta referência é gerada automaticamente de acordo com as normas do estilo IPEN/SP (ABNT NBR 6023) e recomenda-se uma verificação final e ajustes caso necessário.