The radiolabeling of [161Tb]Tb-PSMA-617 by a novel radiolabeling method and preclinical evaluation by in vitro/in vivo methods

IF 1.5 3区化学 Q3 CHEMISTRY, ANALYTICAL Journal of Radioanalytical and Nuclear Chemistry Pub Date : 2024-10-28 DOI:10.1007/s10967-024-09809-8

Emre Uygur, Ceren Sezgin, Yasemin Parlak, Kadriye Buşra Karatay, Bilal Arıkbaşı, Uğur Avcıbaşı, Türkay Toklu, Sabri Barutça, Coşkun Harmanşah, Tevfik Sinan Sözen, Stephan Maus, Howard Scher, Omer Aras, Fikriye Gül Gümüşer, Fazilet Zumrut Biber Muftuler

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引用次数: 0

Abstract

Prostate cancer (PC) is the most prevalent cancer in elderly men, exhibiting a positive correlation with age. As resistance to treatment has developed, particularly in the progressive stage of the disease and in the presence of microfocal multiple bone metastases, new generation radionuclide therapies have emerged. Recently introduced for treating micrometastatic foci, Terbium-161 ([¹⁶¹Tb]) has shown great promise in prostate cancer treatment. This study investigated the in vitro and in vivo cytotoxicity of Terbium-161 ([¹⁶¹Tb])-radiolabeled prostate-specific membrane antigen (PSMA)-617. [¹⁶¹Tb]Tb-PSMA-617 (7.4 MBq/nmol) demonstrated a radiochemical yield of 97.99 ± 2.01% and hydrophilicity. [¹⁶¹Tb]Tb-PSMA-617 was also shown to have good stability, with a radiochemical yield of over 95% up to 72 h. In vitro, [¹⁶¹Tb]Tb-PSMA-617 exhibited cytotoxicity on LNCaP cells but not on PC3 cells. In vivo, scintigraphy imaging visualized the accumulation of [¹⁶¹Tb]Tb-PSMA-617 in the prostate, kidneys, and bladder. The results suggest that [¹⁶¹Tb]Tb-PSMA-617 can be an effective radiolabeled agent for the treatment of PSMA positive foci in prostate cancer.

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来源期刊

Journal of Radioanalytical and Nuclear Chemistry 化学-分析化学

CiteScore

2.80

自引率

18.80%

发文量

504

审稿时长

2.2 months

期刊介绍： An international periodical publishing original papers, letters, review papers and short communications on nuclear chemistry. The subjects covered include: Nuclear chemistry, Radiochemistry, Radiation chemistry, Radiobiological chemistry, Environmental radiochemistry, Production and control of radioisotopes and labelled compounds, Nuclear power plant chemistry, Nuclear fuel chemistry, Radioanalytical chemistry, Radiation detection and measurement, Nuclear instrumentation and automation, etc.