^(89)Zr标记单克隆抗体药物的研究进展  

The Research Progress of Monoclonal Antibody Labeled with^(89)Zr

作　　者：肖展雄 段菲 李洪玉 XIAO Zhanxiong;DUAN Fei;LI Hongyu(Research and Development Center for Nuclear Technology(Radiopharmaceutical Engineering Transformation)of China Atomic Energy Authority,Beijing 102413,China;Engineering and Technology Research Center for Radiopharmaceuticals of China National Nuclear Corporation,Beijing 102413,China;HTA Co.,Ltd.,Beijing 102413,China)

机构地区：[1]国家原子能机构核技术(放射性药物工程转化)研发中心,北京102413 [2]中核集团放射性药物工程技术研究中心,北京102413 [3]原子高科股份有限公司,北京102413

出　　处：《同位素》2025年第2期195-205,共11页Journal of Isotopes

摘　　要：锆-89(^(89)Zr)是一种金属正电子核素,具有较长的半衰期和适中的能量,同时可以通过低能量回旋加速器得到高纯度的^(89)Zr,适用于正电子发射计算机断层显像(PET),尤其成为大分子生物活性物质如抗体标记的核素理想选择。近年来,依托于单克隆抗体药物的发展,^(89)Zr标记单抗药物的研究取得了显著进展,目前已有部分药物进入临床Ⅱ期、Ⅲ期阶段。在标记方法上,^(89)Zr最常用的螯合剂为去铁胺(DFO),已应用于临床,但研究者们仍在不断探索更优的配体。在螯合剂与单抗偶联技术方面,不同形式的DFO衍生物仍是主要研究对象。本文介绍了^(89)Zr的标记方法、螯合剂偶联技术以及^(89)Zr标记单抗类药物的研究进展,并对该类药物所面临的问题与挑战,以及未来发展前景进行分析和展望。Zirconium-89(^(89)Zr)is a metallic positron-emitting radionuclide.The relatively long halflife and moderate energy making^(89)Zr especially suitable for the labeling of large biomolecules such as antibodies for radioimmuno-PET(positron emission tomography)imaging.In recent years,significant progress has been made in the research of^(89)Zr-labeled monoclonal antibodies(mAbs),driven by the development of mAb therapies.Currently,some of these mAb drugs have entered clinical phases II and III.In the labeling methods of^(89)Zr,deferoxamine B(DFO)is the most commonly used chelator and has been applied in clinical research.However,researchers are still continually exploring better ligands.In terms of chelator-mAb conjugation techniques,various forms of DFO derivatives remain the primary focus of research.In this article,^(89)Zr labeling methods,chelator conjugation techniques,and advances in^(89)Zr-mAbs were reviewed.The challenges,issues,and future trends of^(89)Zr-mAbs has also been discussed and prospected.

关 键 词：^(89)Zr 单克隆抗体 正电子发射断层显像(PET) 

分 类 号：TL923[核科学技术—核燃料循环与材料] R187.9[医药卫生—流行病学]