Development of PSMA-targeting neutron capture tharapy based theranostics

2023 Fiscal Year Final Research Report

• Project/Area Number: 21K09339
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Review Section: Basic Section 56030:Urology-related
• Research Institution: Hirosaki University
• Principal Investigator: Yoneyama Tohru 弘前大学, 医学研究科, 助教 (50587649)
• Co-Investigator(Kenkyū-buntansha): 畠山 真吾 弘前大学, 医学研究科, 教授 (10400136) ; 山本 勇人 弘前大学, 医学研究科, 准教授 (30532759) ; 大山 力 弘前大学, 医学研究科, 特任教授 (80282135)
• Project Period (FY): 2021-04-01 – 2024-03-31
• Keywords: MRI / PSMA / 中性子捕捉療法 / Theranostics

Outline of Final Research Achievements

A paradigm shift in the treatment of metastatic castration-resistant prostate cancer is occurring with theranostics modalities that enable simultaneous diagnostic imaging and treatment, such as internal radiation therapy using 177Lu-PSMA-617, a combination of prostate-specific membrane antigen ligand and radioisotope 177Lu. In this study, we aimed to establish image-guided boron neutron capture therapy targeting PSMA as a prostate cancer-specific theranostics modality with low radiation exposure and high therapeutic efficacy. As a result, we synthesized a peptide boron drug consisting of a PSMA-targeting peptide and a boron-10 drug, and found that the boron-accumulating activity was 2-5.4 -fold higher than that of existing boron drugs in prostate cancer-bearing mice.

Free Research Field

糖鎖生物学

Academic Significance and Societal Importance of the Research Achievements

すでに欧米諸国で使用されている177Lu-PSMA-617に代表される前立腺癌特異的TheranosticsはPET/CTおよび放射性同位体を使用するため、被曝の問題から本邦では未承認である。本研究で確立された前立腺癌PSMA標的ペプチドホウ素薬剤に造影効果を示す薬剤を付与することができれば、前立腺癌特異的病変の検出が可能となり、ホウ素中性子捕捉療法による前立腺癌特異的なTheranosticsの確立につながり、前立腺癌治療のbreakthroughになり得る臨床的、社会的に非常に意義が高いと研究と考えられる。