Development of somatostatin based radiopharmaceuticals for receptor mediated radionuclide therapy

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Comparative Evaluation of Therapeutic Radiopharmaceuticals

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The paper describes the methodology used for and the results of labelling [Tyr3 ]octreotate (TATE) with radioiodine (131I) and [DOTA,Tyr3 ]octreotate (DOTATATE) with 131I and lutetium (177Lu). The quality control and purification procedures are also described. Biodistribution studies were performed in normal Swiss mice and in nude mice bearing AR42J tumours. In vitro studies were used to evaluate the affinity of the radiopharmaceuticals for somatostatin receptors in rat brain cortex and tumour cells. Saturation binding and the internalization of the labelled peptides were determined. The frequency of micronuclei in peripheral blood lymphocytes exposed to different radioactive concentrations of [131I]DOTATATE and [ 177Lu]DOTATATE was evaluated by micronucleus assay.

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ARAUJO, E.B.; CALDEIRA FILHO, J.S.; NAGAMATI, L.T.; MURAMOTO, E.; COLTURATO, M.T.; COUTO, R.; OKASAKI, K.; SUZUKI, M.F.; GUIMARAES, M.I.C.C. Development of somatostatin based radiopharmaceuticals for receptor mediated radionuclide therapy. Comparative Evaluation of Therapeutic Radiopharmaceuticals. p. 27-52. Disponível em: http://repositorio.ipen.br/handle/123456789/23066. Acesso em: 20 Mar 2026.
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