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确定基于d-的放射性追踪剂的多价值效应

Siqi Zhang¹, Xiaona Sun¹, Wenhao Liu¹

¹State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Chemical & biomedical imaging

|March 28, 2025

概括

D-多量体显示瘤吸收和脏保留的增加,与L-不同. 这项研究探讨了稳定的放射性药品的d-多元化.

科学领域:

放射性药物开发放射性药物开发
类化学类化学
生物医学成像技术生物医学成像技术

背景情况:

德克斯特罗 (d) 对酶降解具有卓越的稳定性,使其成为放射性药物应用的前景.
多元化增强L-放射性药物的*in vivo*性能,但其对d-类型的作用还未得到充分研究.

研究的目的:

研究多元化对针对PD-L1.1的d-基放射性药物的*in vivo*行为的影响.
为了比较单质,二质和三质d-的药理动力学和生物分布.

主要方法:

合成d-DPA及其二聚体 (DP2) 和三聚体 (DP3).
在正常和瘤携带的小鼠中,对[68Ga]DPA,[68Ga]DP2和[68Ga]DP3进行PET/CT成像和*ex vivo*生物分布研究.

主要成果:

瘤吸收和脏保留随着价值增加 ([⁶⁸Ga]DP3 > [⁶⁸Ga]DP2 > [⁶⁸Ga]DPA).
在肝脏,心脏,肺部,脏,肠道或骨中没有观察到吸收的显著差异.
与单体和二元相比,更高的价值 (三元) 导致血液放射性降低.

结论:

D-的多元化显著影响*体内*的特征,与L-的行为不同.
状结构和链接化学是d-多重体命运的关键因素.
这些发现促进了对镜像相互作用的理解,用于新型放射性药物开发.

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