TY - JOUR

T1 - Preparation and Characterization of 161TB-DOTA-PSMA-617 Using a New Cell Model

AU - Shashkova, O.

AU - Verlov, N.

AU - Avrov, K.O.

AU - Soloveva, S.V.

AU - Terekhina, L.

AU - Pinevich, A.

AU - Shatik, S.

AU - Zaicev, V.V.

AU - Furkina, E.B.

AU - Nadporozskiy, M.A.

AU - Burdakov, V.

AU - Kulakov, I.

AU - Shtam, T.

AU - Stanzevskiy, A.A.

AU - Samoylovich, M.P.

AU - Konevega, A.

N1 - Export Date: 01 November 2025; Cited By: 0; Correspondence Address: O.A. Shashkova; Granov Russian Research Center for Radiology and Surgical Technologies, Ministry of Health of the Russian Federation, St. Petersburg, Russian Federation; email: ujinolga@yandex.ru

PY - 2024

Y1 - 2024

N2 - Terbium-161 is a radioisotope characterized by β-emission, emission of Auger electrons, conversion electrons, and, to a lesser extent, gamma and X-rays. Tb-161 radioconjugate with the DOTA-PSMA-617 ligand (considered as a promising drug for radiotherapy of prostate cancer) was synthesized on the basis of components produced in Russian Federation. The physicochemical characteristics of 161Tb-DOTA-PSMA-617 were investigated. The ability of the radioconjugate to bind to cell membrane receptor was studied on cell line in vitro and in mice in vivo using a new CT26-PSMA cell model representing genetically modified mouse carcinoma cells expressing human PSMA. The pharmacokinetics and biodistribution of the radioconjugate were investigated. The radiopharmaceutical demonstrated highly specific accumulation in the tumor expressing human PSMA unlike in the control tumor. It was not significantly accumulated in the kidneys and other animals’ organs. The blood half-life time of the radiopharmaceutical was determined as 38.4 min. Thus, according to the main criteria, the synthesized radioconjugate 161Tb-DOTA-PSMA-617 is a promising radiopharmaceutical for the treatment of prostate cancer. © 2025 Elsevier B.V., All rights reserved.

AB - Terbium-161 is a radioisotope characterized by β-emission, emission of Auger electrons, conversion electrons, and, to a lesser extent, gamma and X-rays. Tb-161 radioconjugate with the DOTA-PSMA-617 ligand (considered as a promising drug for radiotherapy of prostate cancer) was synthesized on the basis of components produced in Russian Federation. The physicochemical characteristics of 161Tb-DOTA-PSMA-617 were investigated. The ability of the radioconjugate to bind to cell membrane receptor was studied on cell line in vitro and in mice in vivo using a new CT26-PSMA cell model representing genetically modified mouse carcinoma cells expressing human PSMA. The pharmacokinetics and biodistribution of the radioconjugate were investigated. The radiopharmaceutical demonstrated highly specific accumulation in the tumor expressing human PSMA unlike in the control tumor. It was not significantly accumulated in the kidneys and other animals’ organs. The blood half-life time of the radiopharmaceutical was determined as 38.4 min. Thus, according to the main criteria, the synthesized radioconjugate 161Tb-DOTA-PSMA-617 is a promising radiopharmaceutical for the treatment of prostate cancer. © 2025 Elsevier B.V., All rights reserved.

KW - Animal cell culture

KW - Batch cell culture

KW - Cell membranes

KW - Controlled drug delivery

KW - Gamma rays

KW - Metabolism

KW - Pharmacokinetics

KW - Terbium alloys

KW - Auger electron

KW - Cell lines

KW - Conversion electrons

KW - In-vitro

KW - Membrane receptors

KW - New cell model

KW - Physicochemical characteristics

KW - Prostate cancers

KW - Russian federation

KW - Synthesised

KW - Mammals

U2 - 10.1134/S2635167624602808

DO - 10.1134/S2635167624602808

M3 - статья

VL - 19

SP - S218-S225

JO - Nanobiotechnology Reports

JF - Nanobiotechnology Reports

SN - 2635-1676

IS - Suppl 1

ER -