Department of Nuclear Medicine, Institute of Clinical Nuclear Medicine, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China.
Departments of Radiology and Medical Physics, University of Wisconsin-Madison, Madison, Wisconsin.
J Nucl Med. 2022 Oct;63(10):1475-1479. doi: 10.2967/jnumed.122.263907. Epub 2022 Jul 14.
Single-domain antibody (sdAb) is among the most promising vectors for developing molecular imaging tracers. Several sdAb tracers targeting human epidermal growth factor receptor 2 or programmed death ligand 1 have entered clinical practice. However, radiolabeled single-valent sdAbs generally have high kidney retention, limiting their therapeutic applications. Therefore, engineering strategies such as PEGylation or incorporation of renal cleavable linkers can be adapted to improve pharmacokinetics and reduce kidney retention. In this Focus on Molecular Imaging review, we try to summarize the latest developments in sdAb-derived agents and propose potential strategies that can be used to improve the theranostic value of radiolabeled sdAbs.
单域抗体 (sdAb) 是开发分子成像示踪剂最有前途的载体之一。几种针对人表皮生长因子受体 2 或程序性死亡配体 1 的 sdAb 示踪剂已进入临床实践。然而,放射性标记的单价 sdAbs 通常具有较高的肾脏保留,限制了它们的治疗应用。因此,可以采用工程策略,如聚乙二醇化或掺入肾可裂解的连接子,以改善药代动力学并减少肾脏保留。在这篇分子成像综述中,我们试图总结 sdAb 衍生制剂的最新进展,并提出可以用于提高放射性标记 sdAbs 的治疗价值的潜在策略。