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

BOAS, CRISTIAN A.W.V.SILVA, JEFFERSON de J.DIAS, LUIS A.P.FREIRE, MARIA R.B.BALIEIRO, LUIZA M.SANTOS, CAROLINA S.F. dosVIVALDINI, BIANCA F.BENEDETTO, RAQUELVIEIRA, DANIEL P.PASSOS, PRISCILA de Q.S.MARUMO, MARIA H.TEIXEIRA, LUIS F.S.ARAUJO, ELAINE B. de2022-04-132022-04-132022BOAS, CRISTIAN A.W.V.; SILVA, JEFFERSON de J.; DIAS, LUIS A.P.; FREIRE, MARIA R.B.; BALIEIRO, LUIZA M.; SANTOS, CAROLINA S.F. dos; VIVALDINI, BIANCA F.; BENEDETTO, RAQUEL; VIEIRA, DANIEL P.; PASSOS, PRISCILA de Q.S.; MARUMO, MARIA H.; TEIXEIRA, LUIS F.S.; ARAUJO, ELAINE B. de. In vitro and in vivo response of PSMA-617 radiolabeled with CA and NCA lutetium-177. <b>Applied Radiation and Isotopes</b>, v. 180, p. 1-7, 2022. DOI: <a href="https://dx.doi.org/10.1016/j.apradiso.2021.110064">10.1016/j.apradiso.2021.110064</a>. Disponível em: http://repositorio.ipen.br/handle/123456789/32952.0969-8043http://repositorio.ipen.br/handle/123456789/32952The PSMA-targeted radionuclide therapy has been explored since 2015 with radioisotope lutetium-177, whose β− 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 177Lu-PSMA-617. The influence of the specific activity of lutetium-177 on the properties of the radiopharmaceutical PSMA-617 was evaluated through pre-clinical 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 177Lu-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.1-7openAccessprostatemembranesantigenslutetium 177activity levelsin vivoin vitroin vitroradiopharmaceuticalsneoplasmsIn vitro and in vivo response of PSMA-617 radiolabeled with CA and NCA lutetium-177Artigo de periódico18010.1016/j.apradiso.2021.1100640000-0002-0007-534Xhttps://orcid.org/0000-0003-0456-5589https://orcid.org/0000-0003-2852-6189https://orcid.org/0000-0002-0007-534X32.546