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Molecular pharmaceutics. 2025 Jun 10. doi: 10.1021/acs.molpharmaceut.5c00214 Q14.52025

In Vitro and In Vivo Study of Novel PSMA-Targeted Radioligands: Enhancing Tumor Uptake and Therapeutic Efficacy through Zwitterionization and Albumin-Binding Strategies

新型PSMA靶向放射配体的体内外研究：通过两性离子化和白蛋白结合策略增强肿瘤摄取和治疗疗效 翻译改进

Yang Liu  1  2  3, Haiyang Li  1  2  4, Han Zhou  5, Hongmei Yuan  1  2  4, Yan Zhao  1  2  3, Zhicong Yang  1  2  4, Sufan Tang  1  2  4, Tongtong Wu  1  2  4, Li Wang  1  2  3  4, Zhanwen Huang  1  2  3, Yue Chen  1  2  3, Nan Liu  6, Zhijun Zhou  1  2  3  4

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作者单位

  • 1 Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Jiangyang District, Luzhou 646000, Sichuan, China.
  • 2 Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Jiangyang District, Luzhou 646000, Sichuan, China.
  • 3 Institute of Nuclear Medicine, Southwest Medical University, Jiangyang District, Luzhou 646000, Sichuan, China.
  • 4 Department of Pharmaceutics, School of Pharmacy, Southwest Medical University, Jiangyang District, Luzhou 646000, Sichuan, China.
  • 5 Faculty of Nursing, University of Windsor, Windsor N9B 3P4, Ontario, Canada.
  • 6 Department of Nuclear Medicine, Sichuan Provincial People's Hospital, University of Electronic Science and Technology of China, Chengdu 611731, Sichuan, China.

    • DOI: 10.1021/acs.molpharmaceut.5c00214 PMID: 40494649

    摘要 中英对照阅读

    Prostate-specific membrane antigen (PSMA) targeted radioligand therapy (TRT) for metastatic castration-resistant prostate cancer has demonstrated significant potential. This study aimed to develop an optimal radiotherapeutic agent suitable for high-level PSMA expression by optimizing the ligand structure with albumin-binding zwitterionic strategies to increase tumor uptake and retention time and to explore the effects of these strategies on the in vitro an... ...点击完成人机验证后继续浏览

    特异性膜抗原（PSMA）靶向放射配体治疗（TRT）在转移性去势抵抗性前列腺癌中显示出巨大的潜力。本研究旨在通过优化配体结构并采用与白蛋白结合的两性离子策略，开发出适用于高表达PSMA的最优放疗剂，以增加肿瘤摄取和滞留时间，并探讨这些策略对PSMA抑制剂体内和体外性质的影响。所有前体均基于PSMA靶向药物Flu-1合成。通过镓和镥标记来评估放射配体的理化性质、成像及生物分布，进而评价其药代动力学特性以及与PSMA的亲和力和特异性。以177Lu标记的Flu-1、BWD、P4-BWD和P4-PND的放射配体系统地评估了治疗效果。@All PSMA ligands were of chemical purity >95%. The final radiochemical purity of the radioligands was achieved up to 99%.细胞研究及成像结果显示，BWD对PSMA具有高亲和力（IC50=35.86±0.56），在肿瘤摄取与滞留方面显著优于其他放射配体。@The biodistribution study further confirmed that the tumor uptake of 177Lu-BWD (64.28 ± 12.46%ID/g) was significantly higher than that of other 177Lu-radioligands at 4 h postinjection, including 177Lu-PSMA-617 (47.64 ± 11.39%ID/g). TRT结果显示，单次注射7.4 MBq的177Lu-BWD显著抑制了PC3-PIP肿瘤生长，在相同条件下优于177Lu-PSMA-617。@177Lu-BWD with greatly enhanced tumor uptake and retention demonstrated remarkable therapeutic efficacy using significantly lower dosages for clinical translation to treat PCa with high level of PSMA expression.

    关键词： PSMA；白蛋白结合；前列腺癌；靶向放射配体治疗；两性离子化。

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    期刊名：Molecular pharmaceutics

    缩写：MOL PHARMACEUT

    ISSN：1543-8384

    e-ISSN：1543-8392

    IF/分区：4.5/Q1

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    In Vitro and In Vivo Study of Novel PSMA-Targeted Radioligands: Enhancing Tumor Uptake and Therapeutic Efficacy through Zwitterionization and Albumin-Binding Strategies