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<p>The paper presents the results of investigating three new PSMA-molecules: PSMA-BQ7876, PSMA-D1, and PSMA-D2, which are considered as ligands for targeted radionuclide therapy of metastatic castration-resistant prostate cancer. Beta-emitting lutetium-177 radionuclide obtained by the activation method from an ytterbium target (Yb-176) in the reactor neutron flux is considered as a drug agent in the ligand composition. The investigations were conducted using the method of direct comparative analysis in which a PSMA-617 molecule-based drug was selected as a pharmaceutical prototype. An assessment has been made of the specificity and cytotoxic activity of PSMA-complexes with respect to tumor cells: cells hyperexpressing a PSMA-antigen (22RV1 cell culture) and cells with low PSMA expression (PC3 cell cultures).</p>

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Comparative Analysis of Promising Antineoplastic Drugs for Prostate Carcinoma Therapy in in vitro Experiments

  • 期刊论文

  • 发表日期：

    2025年11月28日

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  • K. A. Makoveeva,
  • A. V. Kurochkin,
  • K. V. Kokov,
  • A. V. Kolotaev,
  • V. N. Osipov,
  • A. A. Pankratov,
  • A. D. Plyutinskaya,
  • D. S. Khachatryan,
  • D. Yu. Chuvilin,
  • M. S. Lar′kina,
  • V. I. Chernov,
  • S. M. Deev,
  • I. N. Zavestovskaya

摘要

The paper presents the results of investigating three new PSMA-molecules: PSMA-BQ7876, PSMA-D1, and PSMA-D2, which are considered as ligands for targeted radionuclide therapy of metastatic castration-resistant prostate cancer. Beta-emitting lutetium-177 radionuclide obtained by the activation method from an ytterbium target (Yb-176) in the reactor neutron flux is considered as a drug agent in the ligand composition. The investigations were conducted using the method of direct comparative analysis in which a PSMA-617 molecule-based drug was selected as a pharmaceutical prototype. An assessment has been made of the specificity and cytotoxic activity of PSMA-complexes with respect to tumor cells: cells hyperexpressing a PSMA-antigen (22RV1 cell culture) and cells with low PSMA expression (PC3 cell cultures).