89Zr标记单克隆抗体药物的研究进展

The Research Progress of Monoclonal Antibody Labeled with 89Zr

  • 摘要: 锆-89(89Zr)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89Zr,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,89Zr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,89Zr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89Zr的标记方法、螯合剂偶联技术以及89Zr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。

     

    Abstract: Zirconium-89 (89Zr) is a metallic positron-emitting radionuclide. The relatively long half-life and moderate energy making 89Zr 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 89Zr-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 89Zr, 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, 89Zr labeling methods, chelator conjugation techniques, and advances in 89Zr-mAbs were reviewed. The challenges, issues, and future trends of 89Zr-mAbs has also been discussed and prospected.

     

/

返回文章
返回