In vitro and in vivo response of PSMA-617 radiolabeled with CA and NCA lutetium-177

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Villas Boas, Cristian Antonio Wieczorek ^{[1, 2]} ; Silva, Jefferson de Jesus ^[1] ; Pereira Dias, Luis Alberto ^[1] ; Brandao Freire, Maria Renata ^[1] ; Balieiro, Luiza Mascarenhas ^[1] ; Ferreira dos Santos, Carolina Silva ^[1] ; Vivaldini, Bianca Franchesqueti ^[1] ; Benedetto, Raquel ^[1] ; Vieira, Daniel Perez ^[1] ; Souza Passos, Priscila de Queiroz ^[1] ; Marumo, Maria Helena ^[1] ; Teixeira, Luis Felipe S. ^[1] ; de Araujo, Elaine Bortoleti ^[1]

Afiliação do(s) autor(es)

^[1] IPEN CNEN, Inst Pesquisas Energet & Nucl, Av Prof Lineu Prestes 2242, Cidade Univ, BR-05508000 Sao Paulo - Brazil

^[2] Washington Univ, Dept Radiat Oncol, Sch Med, 4511 Forest Pk Ave, St Louis, MO 63110 - USA

• Tipo de documento: Artigo Científico
• Fonte: Applied Radiation and Isotopes; v. 180, FEB 2022.
• Citações Web of Science: 0

Resumo

The PSMA-targeted radionuclide therapy has been explored since 2015 with radioisotope lutetium-177, whose beta(-) emission range is adequate for micrometastases treatment. This radioisotope is obtained by two different production routes that directly affect the specific activity of lutetium-177 (non-carrier added and carrier added) and, consequently, the specific activity of radiopharmaceuticals, like Lu-177-PSMA-617. The influence of the specific activity of lutetium-177 on the properties of the radiopharmaceutical PSMA-617 was evaluated through preclinical studies. The in vitro study pointed to a lower constant of dissociation with non-carrier added lutetium-177 due to the difference in the specific activity. However, competition and internalization assays resulted in similar results for both lutetium-177. Based on these pre-clinical experiments, the total in vitro tumor cell binding and tumor uptake in vivo were similar, with no influence of the specific activity of the Lu-177-PSMA-617. Regardless the specific activity did not directly affect tumor uptake, the tumor/non-target organs ratios were higher for the radiopharmaceutical labeled with carrier added lutetium-177, which had the lowest specific activity. (AU)

• Processo FAPESP: 18/12965-4 - Obtenção de kit de PSMA-617 para pronta marcação com lutécio-177 e avaliação da sua aplicabilidade no tratamento do Câncer de Próstata
• Beneficiário: Cristian Antonio Wieczorek Villas Boas
• Modalidade de apoio: Bolsas no Brasil - Doutorado