Suzuki Hiroyuki, Kannaka Kento, Uehara Tomoya
Laboratory of Molecular Imaging and Radiotherapy, Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan.
Pharmaceuticals (Basel). 2024 Apr 16;17(4):508. doi: 10.3390/ph17040508.
Radiolabeled antibodies are powerful tools for both imaging and therapy in the field of nuclear medicine. Radiolabeling methods that do not release radionuclides from parent antibodies are essential for radiolabeling antibodies, and practical radiolabeling protocols that provide high in vivo stability have been established for many radionuclides, with a few exceptions. However, several limitations remain, including undesirable side effects on the biodistribution profiles of antibodies. This review summarizes the numerous efforts made to tackle this problem and the recent advances, mainly in preclinical studies. These include pretargeting approaches, engineered antibody fragments and constructs, the secondary injection of clearing agents, and the insertion of metabolizable linkages. Finally, we discuss the potential of these approaches and their prospects for further clinical application.
放射性标记抗体是核医学领域成像和治疗的强大工具。不使放射性核素从母体抗体中释放出来的放射性标记方法对于抗体放射性标记至关重要，并且已经为许多放射性核素建立了具有高体内稳定性的实用放射性标记方案，但有少数例外。然而，仍然存在一些局限性，包括对抗体生物分布概况的不良副作用。本综述总结了为解决这一问题所做的大量努力以及近期进展，主要是在临床前研究方面。这些包括预靶向方法、工程化抗体片段和构建体、清除剂的二次注射以及可代谢连接键的插入。最后，我们讨论了这些方法的潜力及其进一步临床应用的前景。
