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对-227向辐射治疗的双功能化剂的合成和评估

Joshua J Woods¹, Alex Rigby¹, Jennifer N Wacker¹

¹Chemical Sciences Division, Lawrence Berkeley National Laboratory, Berkeley, California 94720, United States.

Journal of medicinal chemistry

|January 3, 2025

概括

一种新的双功能化剂,p-SCN-Bn-DOTHOPO,简化了使用-227 (227Th) 的化治疗剂的合成. 这种新型化剂还可以使用-89 (89Zr) 进行成像应用.

科学领域:

放射化学放射化学是指辐射化学.
核医学是一种核医学.
免疫结合体的发展

背景情况:

-227 (227Th) 是针对性阿尔法疗法的有前途的阿尔法发射体.
现有的227Th化剂需要复杂的,多步骤的合成.
开发高效的化剂对于推进基于227Th的放射性药物至关重要.

研究的目的:

为了合成和评估一个新的双功能化剂,p-SCN-Bn-DOTHOPO,为227Th和89Zr.
为了将化剂与向抗体 (trastuzumab) 相结合.
评估产生的免疫结合物的放射标记效率,纯度和稳定性.

主要方法:

通过四步过程合成p-SCN-Bn-DOTHOPO.
化剂的结合与特拉斯图祖马布.
用227Th和89Zr进行放射性标记.
评估放射性化学产量,纯度和生物稳定性.

主要成果:

新型双功能化剂p-SCN-Bn-DOTHOPO的合成总产量为26%.
免疫结合物被有效地标记为227Th (≥95%的产量和纯度) 和89Zr.
放射性金属复合物表现出良好的生物稳定性.

结论:

p-SCN-Bn-DOTHOPO为开发227Th和89Zr放射性药物提供了一种简化方法.
这种化剂有助于创建下一代向阿尔法疗法和PET成像剂.
这些发现为放射性金属复合的化器设计提供了宝贵的见解.

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