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

Overview

Journal Res Sq

Date 2023 Nov 14

PMID 37961521

Authors

Emre Uygur

Ceren Sezgin

Yasemin Parlak

Kadriye Busra Karatay

Bilal Arikbasi

Ugur Avcibasi

Turkay Toklu

Sabri Barutca

Coskun Harmansah

Tevfik Sinan Sozen

Stephan Maus

Howard Scher

Omer Aras

Fikriye Gul Gumuser

Fazilet Zumrut Biber Muftuler

Affiliations

Soon will be listed here.

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, [Tb], a radiolanthanide introduced for treating micrometastatic foci, has shown great promise for treating prostate cancer.

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

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

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