Development of a Novel PSMA-Targeted Radiopharmaceutical - Strategy for Bioequivalence between 18F and 211At

2022 Fiscal Year Final Research Report

• Project/Area Number: 20K16732
• Research Category: Grant-in-Aid for Early-Career Scientists
• Allocation Type: Multi-year Fund
• Review Section: Basic Section 52040:Radiological sciences-related
• Research Institution: Fukushima Medical University
• Principal Investigator: Joho Taiki 福島県立医科大学, 公私立大学の部局等, 助手 (40848876)
• Project Period (FY): 2020-04-01 – 2023-03-31
• Keywords: PSMA / アスタチン211

Outline of Final Research Achievements

In the first year, I achieved the synthesis of NH-GKP-PSMA and B(pin)-Ph-COOt-Bu, which are the synthetic precursors for labeling 18F (211At)-BzGKP-PSMA, and I-BzGKP-PSMA, which is an iodide compound. In the next year, I achieved the investigation of deprotection conditions for B(pin)-Ph-COOt-Bu and the development of an efficient synthetic method for BzGKP-PSMA. In the final year, improvement of the yield of I-BzGKP-PSMA was achieved. The labeled precursor B(pin)-BzGKP-PSMA-Resin was also synthesized and the labeling with 211At was investigated. The labeling reaction did not occur if the Resin residue was left intact.

Free Research Field

ラジオセラノスティクス

Academic Significance and Societal Importance of the Research Achievements

本研究では、PSMA発現腫瘍に特異的に集積する新規放射性薬剤(211At-BzGKP-PSMA)を設計し、その類似化合物であるI-BzGKP-PSMAの合成を達成した。さらにB(pin)-BzGKP-PSMA-Resinの合成を達成し、それにアルファ線放出核種である211Atの標識検討を行った。いずれも標識反応は進行しなかったため、今後更なる検討を行い、難治性であり、QOLの悪い転移性去勢抵抗性前立腺癌 (mCRPC)の患者への新規治療薬を開発する。