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[Preprint]. 2023 Oct 30:rs.3.rs-3415703.
doi: 10.21203/rs.3.rs-3415703/v1.

The Radiolabeling of [161Tb]-PSMA-617 by a Novel Radiolabeling Method and Preclinical Evaluation by In Vitro/In Vivo Methods

Emre Uygur  1 , Ceren Sezgin  2 , Yasemin Parlak  1 , Kadriye Busra Karatay  3 , Bilal Arikbasi  2 , Ugur Avcibasi  4 , Turkay Toklu  5 , Sabri Barutca  6 , Coskun Harmansah  7 , Tevfik Sinan Sozen  8 , Stephan Maus  9 , Howard Scher  10 , Omer Aras  10 , Fikriye Gul Gumuser  1 , Fazilet Zumrut Biber Muftuler  3
Affiliations

The Radiolabeling of [161Tb]-PSMA-617 by a Novel Radiolabeling Method and Preclinical Evaluation by In Vitro/In Vivo Methods

Emre Uygur et al. Res Sq. .

Abstract

Background: Prostate cancer (PC) is the most common type of cancer in elderly men, with 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, [161Tb], a radiolanthanide introduced for treating micrometastatic foci, has shown great promise for treating prostate cancer.

Results: In this study, Terbium-161 [161Tb]Tb was radiolabeled with prostate-specific membrane antigen (PSMA)-617 ([161Tb]-PSMA-617) and the therapeutic efficacy of the radiolabeled compound investigated in vitro and in vivo. [161Tb]-PSMA-617 was found to have a radiochemical yield of 97.99 ± 2.01% and was hydrophilic. [161Tb]-PSMA-617 was also shown to have good stability, with a radiochemical yield of over 95% up to 72 hours. In vitro, [161Tb]-PSMA-617 showed a cytotoxic effect on LNCaP cells but not on PC-3 cells. In vivo, scintigraphy imaging visualized the accumulation of [161Tb]-PSMA-617 in the prostate, kidneys, and bladder.

Conclusions: The results suggest that [161Tb]-PSMA-617 can be an effective radiolabeled agent for the treatment of PSMA positive foci in prostate cancer.

Keywords: PSMA-617; Terbium-161 [161Tb]Tb; prostate cancer.

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Conflict of interest statement

Competing interests None of the authors have a conflict of interest.

Figures

Figure 1.
Figure 1.
TLRC Chromatograms.
Figure 2.
Figure 2.
HPLRC Chromatograms.
Figure 3.
Figure 3.
Stability of the [161Tb]Tb-PSMA-617
Figure 4.
Figure 4.
24 h cell viability graph of [161Tb]Tb-PSMA-617 on PC-3 and LNCaP cell lines.
Figure 5.
Figure 5.
Cell uptake graph of [161Tb]TbCl3 and [161Tb]Tb-PSMA-617(P≤ 0.05).
Figure 6.
Figure 6.
Scintigraphy images in the different time periods of the [161Tb]Tb-PSMA-617
Figure 7.
Figure 7.
Biodistribution of [161Tb]-PSMA-617 On Albino Wistar Rats (n=3)
See this image and copyright information in PMC

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