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
王国昌 1徐鹏飞 2张静静 3陈小元3
作者信息
- 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
- 折叠
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.
Abstract
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 ra-diotheranostics.Evans blue(EB)motif uses endogenous albumin as a reversible carrier,and the small mol-ecule 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Key words
Precision medicine/Radiopharmaceuticals/Evans blue/Trends引用本文复制引用
出版年
2024