摘要
锕-225(^(225)Ac)具有高传能线密度、适宜的半衰期、短粒子射程和良好的配位能力等特性,是很有医用前景的α核素之一,在肿瘤的靶向放射性核素治疗中具有重要的研究价值。本文简要介绍了^(225)Ac的物理和化学特性以及常用螯合剂(前列腺特异性膜抗原、奥曲肽、纳米载体等),围绕着以多肽或小分子为靶向分子、以单克隆抗体或蛋白为靶向分子和基于纳米载体的TAT药物,综述了^(225)Ac标记的靶向药物在肿瘤中的应用和纳米材料对^(225)Ac衰变子体的保留作用,分析其应用于治疗的价值,总结了^(225)Ac标记方法和适宜螯合剂的选择、靶向性的提高、毒副作用,展望了^(225)Ac国产化以满足未来的临床需求,以期为后续的^(225)Ac标记药物研发提供参考。
^(225)Ac has high linear energy transfer,suitable half-life,short particle range,and good coordination ability,making it one of the promising alpha emitters in targeted radioisotope therapy for tumors,and it has significant research value.This article briefly introduces the physical and chemical properties of^(225)Ac,as well as common chelating agents(prostate-specific membrane antigen,octreotide,nano-carriers,etc.).It reviews the applications of targeted drugs labeled with^(225)Ac in tumors,based on peptides or small molecules as targeting agents,monoclonal antibodies or proteins as targeting molecules,and nano-carriers.It also analyzes the value of its application in therapy,summarizes the methods of labeling with^(225)Ac and the selection of suitable chelating agents,improvements in targeting specificity,and toxicity side effects.Furthermore,it looks forward to the localization of^(225)Ac production to meet future clinical needs,in order to provide reference for the subsequent development of^(225)Ac-labeled drugs.
作者
王立琴
柳江燕
WANG Liqin;LIU Jiangyan(Department of Nuclear Medicine,Lanzhou University Second Hospital,Lanzhou 730030,China;The Second Hospital of Lanzhou University,Lanzhou 730030,China)
出处
《中山大学学报（医学科学版）》
CAS
CSCD
北大核心
2024年第4期503-510,共8页
Journal of Sun Yat-Sen University:Medical Sciences
基金
甘肃省科技计划项目(23JRRA569)
兰州大学第二医院“萃英研究生指导教师”培育计划(CYDSPY202001)。
关键词
锕-225
α核素
肿瘤
靶向α治疗
多肽
抗体
纳米载体
Actinium-225
α-emitting radionuclide
tumor
targetedα-therapy
polypeptide
antibody
nanocarrier
作者简介
第一作者:王立琴,研究方向:核素诊断及治疗,E-mail:2282708201@qq.com;通信作者:柳江燕,主任医师,研究方向:核素诊断及治疗,E-mail:Ery_liujy@lzu.edu.cn。
