^(225)Ac在肿瘤靶向治疗中的应用及进展  

Application and Research Progress of^(225)Ac in Tumor Targeted Treatment

作　　者：王立琴 柳江燕[1,2] WANG Liqin;LIU Jiangyan(Department of Nuclear Medicine,Lanzhou University Second Hospital,Lanzhou 730030,China;The Second Hospital of Lanzhou University,Lanzhou 730030,China)

机构地区：[1]兰州大学第二医院核医学科,甘肃兰州730030 [2]兰州大学第二临床医学院,甘肃兰州730030

出　　处：《中山大学学报（医学科学版）》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)。

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.

关 键 词：锕-225 α核素 肿瘤 靶向α治疗 多肽 抗体 纳米载体 

分 类 号：R459.9[医药卫生—治疗学]