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曲妥珠单抗、亲和体和纳米抗体作为药物载体在乳腺癌中的应用,特别关注放射免疫治疗和放射免疫显像。

HER2-directed antibodies, affibodies and nanobodies as drug-delivery vehicles in breast cancer with a specific focus on radioimmunotherapy and radioimmunoimaging.

机构信息

Department of Nuclear Medicine, University Hospital Aachen, RWTH Aachen University, 52074, Aachen, Germany.

Center of Integrated Oncology (CIO), Universities of Aachen, Bonn, Cologne and Düsseldorf, Kerpener Str. 62, 50937, Cologne, Germany.

出版信息

Eur J Nucl Med Mol Imaging. 2021 May;48(5):1371-1389. doi: 10.1007/s00259-020-05094-1. Epub 2020 Nov 12.

Abstract

PURPOSE

The aim of the present paper is to review the role of HER2 antibodies, affibodies and nanobodies as vehicles for imaging and therapy approaches in breast cancer, including a detailed look at recent clinical data from antibody drug conjugates and nanobodies as well as affibodies that are currently under development.

RESULTS

Clinical and preclinical studies have shown that the use of monoclonal antibodies in molecular imaging is impaired by slow blood clearance, associated with slow and low tumor uptake and with limited tumor penetration potential. Antibody fragments, such as nanobodies, on the other hand, can be radiolabelled with short-lived radioisotopes and provide high-contrast images within a few hours after injection, allowing early diagnosis and reduced radiation exposure of patients. Even in therapy, the small radioactively labeled nanobodies prove to be superior to radioactively labeled monoclonal antibodies due to their higher specificity and their ability to penetrate the tumor.

CONCLUSION

While monoclonal antibodies are well established drug delivery vehicles, the current literature on molecular imaging supports the notion that antibody fragments, such as affibodies or nanobodies, might be superior in this approach.

摘要

目的

本文旨在综述 HER2 抗体、亲和体和纳米抗体作为乳腺癌成像和治疗方法载体的作用,包括详细分析当前处于开发阶段的抗体药物偶联物和纳米抗体的最新临床数据。

结果

临床前和临床研究表明,单克隆抗体在分子成像中的应用受到血清除率缓慢的限制,与肿瘤摄取缓慢且低以及肿瘤穿透潜力有限有关。另一方面,抗体片段,如纳米抗体,可以用短半衰期放射性同位素进行放射性标记,并在注射后数小时内提供高对比度图像,从而实现早期诊断和减少患者的辐射暴露。即使在治疗中,由于其更高的特异性和穿透肿瘤的能力,小的放射性标记纳米抗体也优于放射性标记的单克隆抗体。

结论

虽然单克隆抗体是成熟的药物递送载体,但分子成像的现有文献支持这样一种观点,即抗体片段(如亲和体或纳米抗体)在这种方法中可能更具优势。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c79/8113197/a893562197c5/259_2020_5094_Fig1_HTML.jpg

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