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MIB指南:用于临床前癌症成像的[锆]锆-DFO-曲妥珠单抗和[铜]铜-NOTA-曲妥珠单抗

MIB guides: [Zr]Zr-DFO-trastuzumab and [Cu]Cu-NOTA-Trastuzumab for Preclinical Cancer Imaging.

作者信息

Simó Cristina, Vanover Alexander C, Azevedo E Carmen, Pereira Patrícia M R

机构信息

Department of Radiology, Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO, 63110, USA.

Cancer Biology Graduate Program, Washington University School of Medicine, St. Louis, MO, USA.

出版信息

Mol Imaging Biol. 2025 Jun 26. doi: 10.1007/s11307-025-02022-3.

Abstract

Radiopharmaceuticals based on antibody biomolecules are widely used in oncology for positron emission tomography (PET). Trastuzumab, an antibody that targets the epidermal growth factor receptor 2 (HER2), has been extensively studied for both preclinical and clinical cancer imaging. This MIB guide specifically focuses on the radiolabeling of the antibody trastuzumab with zirconium-89 (Zr) and copper-64 (Cu) for PET imaging. The guide describes the steps for conjugating trastuzumab with p-SCN-Bn-deferoxamine (DFO) or 2,2',2''-(1,4,7-triazacyclononane-1,4,7-triyl)triacetic acid (p-SCN-Bn-NOTA) chelators through conjugation between the isothiocyanate (-SCN) functional group on the chelator with lysines on the trastuzumab. We also describe subsequent radiolabeling steps with Zr or Cu. The steps described here can be adapted to the radiolabeling of other antibodies upon protocol optimization.

摘要

基于抗体生物分子的放射性药物在肿瘤学正电子发射断层扫描(PET)中被广泛应用。曲妥珠单抗是一种靶向表皮生长因子受体2(HER2)的抗体,已在临床前和临床癌症成像方面得到广泛研究。本MIB指南特别关注用锆 - 89(Zr)和铜 - 64(Cu)对曲妥珠单抗进行放射性标记以用于PET成像。该指南描述了通过螯合剂上的异硫氰酸酯(-SCN)官能团与曲妥珠单抗上的赖氨酸之间的共轭反应,将曲妥珠单抗与对 - SCN - Bn - 去铁胺(DFO)或2,2',2'' - (1,4,7 - 三氮杂环壬烷 - 1,4,7 - 三基)三乙酸(对 - SCN - Bn - NOTA)螯合剂进行共轭的步骤。我们还描述了随后用Zr或Cu进行放射性标记的步骤。这里描述的步骤经方案优化后可适用于其他抗体的放射性标记。

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