Optimization of PSMA-I&T radiolabeling with 177Lu
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 a...
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| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Brazilian Radiation Protection Society (Sociedade Brasileira de Proteção Radiológica, SBPR)
2025-06-01
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| Series: | Brazilian Journal of Radiation Sciences |
| Subjects: | |
| Online Access: | https://bjrs.org.br/revista/index.php/REVISTA/article/view/2690 |
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| Summary: | 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. 177 Lu-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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| ISSN: | 2319-0612 |