Optimization of PSMA-I&T radiolabeling with 177Lu

Luiza Mascarenhas Balieiro; Maria das Dores Domingos; Luana Pereira da Silva; Joel Mendes dos Santos; Margareth Mie Nakamura Matsuda; Luis Alberto Pereira Dias; Elaine Bortoleti de Araújo

doi:10.15392/2319-0612.2024.2690

Autores/as

Luiza Mascarenhas Balieiro IPEN https://orcid.org/0000-0002-4293-6347 (no autenticado)
Maria das Dores Domingos IPEN
Luana Pereira da Silva IPEN
Joel Mendes dos Santos IPEN
Margareth Mie Nakamura Matsuda IPEN https://orcid.org/0000-0003-4455-3486 (no autenticado)
Luis Alberto Pereira Dias IPEN https://orcid.org/0009-0008-3228-6409 (no autenticado)
Elaine Bortoleti de Araújo IPEN https://orcid.org/0000-0003-0456-5589 (no autenticado)

DOI:

https://doi.org/10.15392/2319-0612.2024.2690

Palabras clave:

Radiolabeling 1, PSMA I&T 2, Optimization 3, Lutetium-177 4

Resumen

Prostate cancer (PCa) is the second most common type of cancer in men and the fifth cause of mortality worldwide. Metastatic prostate cancer is associated with a poor prognosis and decreased life expectancy. Prostate-specific membrane antigen (PSMA) is a type II transmembrane glycoprotein that is anchored in the epithelial prostate cell membrane, overexpressed in prostate cancer, increased in metastatic castration-resistant prostate cancer (mCRPC) patients and with a consensus that its expression level is correlated to the malignancy of the disease. ¹⁷⁷Lu-PSMA-I&T stands out as a promissor radiopharmaceutical for therapy of prostate cancer and currently is being described based on this specifically bind to PSMA with the Glu-urea-Lys pharmacophoric group. This present work aimed to determine the most favorable conditions for labeling PSMA I&T with carried-added lutetium-177, evaluating the influence of molar ratio, pH, temperature and reaction time, to obtain the radiopharmaceutical with high radiochemical purity (%RP ≥95%), avoiding the final purification step. The percentage of radiochemical purity was evaluated by High Pressure Liquid Chromatography (HPLC) and Thin Layer Chromatography on silica gel 60 plate (TLC-SG). The results obtained with this work made it possible to define and standardize the best condition for PSMA I&T radiolabeling with carried-added ¹⁷⁷Lu.

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