伊文思蓝改构放射性药物在诊疗一体化中的应用进展  

Application progress of Evans blue modified radiopharmaceuticals for theranostics

作　　者：王国昌 徐鹏飞 张静静 陈小元 Wang Guochang;Xu Pengfei;Zhang Jingjing;Chen Xiaoyuan(Department of Nuclear Medicine,Peking Union Medical College Hospital,Peking Union Medical College,Chinese Academy of Medical Sciences State Key Laboratory of Complex Severe and Rare Disease Beijing Key Laboratory of Molecular Targeted Diagnosis and Therapy in Nuclear Medicine,Beijing 100730,China;Translational Pharmaceutical Laboratory,Jining First People′s Hospital,Shandong First Medical University,Jining 272000,China;Yong Loo Lin School of Medicine and Faculty of Engineering,National University of Singapore,Singapore 119074,Singapore)

机构地区：[1]中国医学科学院、北京协和医学院北京协和医院核医学科、疑难重症及罕见病国家重点实验室、核医学分子靶向诊疗北京市重点实验室,北京100730 [2]山东第一医科大学附属济宁第一人民医院转化药学实验室,济宁272000 [3]新加坡国立大学杨潞龄医学院/工程学院,新加坡119074

出　　处：《中华核医学与分子影像杂志》2024年第1期35-40,共6页Chinese Journal of Nuclear Medicine and Molecular Imaging

摘　　要：核医学诊疗一体化是精准医学发展的重要方向。基于小分子/多肽的放射性核素治疗往往需要较高剂量。提高核素的使用效率、延长核素治疗型分子探针的体内代谢、增加靶/非靶比值, 成为了国内外研究的热点前沿。利用与白蛋白高亲和力的截断型伊文思蓝(EB)对多肽核素药物进行修饰, 可延长其半衰期, 增加靶病灶对放射性药物的摄取和放射性药物在靶病灶的滞留, 从而提高疗效并降低核素使用剂量。该文将围绕EB改构放射性药物用于诊疗一体化的研究进行概述。Theranostics in nuclear medicine is an important direction for the precision medicine.Radionuclide therapy based on small molecules/peptides often requires high doses.Improving the utilization efficiency of radionuclides,optimizing the pharmacokinetics of radionuclide therapeutic molecular probes as well as increasing the target to non-target ratio have become the international hot frontiers in the field of radiotheranostics.Evans blue(EB)motif uses endogenous albumin as a reversible carrier,and the small molecule and polypeptide structure modified based on EB can effectively extend the half-life in the blood and substantially increase the uptake,accumulation and retention of radiopharmaceuticals in target lesions,and thereby enhance the therapeutic effect and reduce the dosage of nuclides.This article focuses on the research of EB modified radiopharmaceuticals for theranostics.

关 键 词：精准医学 放射性药物 伊文思蓝 发展趋势 

分 类 号：R817[医药卫生—影像医学与核医学]