Li Zuojie, Ruan Qing, Jiang Yuhao, Wang Qianna, Yin Guangxing, Feng Junhong, Zhang Junbo
Key Laboratory of Radiopharmaceuticals of the Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing 100875, P. R. China.
Key Laboratory of Beam Technology of the Ministry of Education, College of Physics and Astronomy, Beijing Normal University, Beijing, 100875, P. R. China.
J Med Chem. 2024 Dec 26;67(24):21644-21670. doi: 10.1021/acs.jmedchem.4c01608. Epub 2024 Dec 8.
Radiotracers provide molecular- and cellular-level information in a noninvasive manner and have become important tools for precision medicine. In particular, the successful clinical application of radioligand therapeutic (RLT) has further strengthened the role of nuclear medicine in clinical treatment. The complicated microenvironment of the lesion has rendered traditional single-targeted radiopharmaceuticals incapable of fully meeting the requirements. The design and development of dual-targeted and multitargeted radiopharmaceuticals have rapidly emerged. In recent years, significant progress has been made in the development of heterologous dual-targeted radiopharmaceuticals. This perspective aims to provide a comprehensive overview of the recent progress in these heterologous dual-targeted radiopharmaceuticals, with a special focus on the design of ligand structures, pharmacological properties, and preclinical and clinical evaluation. Furthermore, future directions are discussed from this perspective.
放射性示踪剂以非侵入性方式提供分子和细胞水平的信息，已成为精准医学的重要工具。特别是，放射性配体治疗（RLT）的成功临床应用进一步强化了核医学在临床治疗中的作用。病变复杂的微环境使得传统的单靶点放射性药物无法完全满足需求。双靶点和多靶点放射性药物的设计与开发迅速涌现。近年来，异源双靶点放射性药物的开发取得了显著进展。本文旨在全面概述这些异源双靶点放射性药物的最新进展，特别关注配体结构设计、药理学特性以及临床前和临床评估。此外，还从这一角度讨论了未来的发展方向。
