放射性核素偶联药物（RDCs）是一类将放射性同位素与药物分子结合的化合物，该类药物在体内起效时会借助其独有的内照射有效杀伤肿瘤细胞，且具有远端效应以及旁观者效应，在治疗扩散性肿瘤时具有较大应用潜力。根据所结合的核素用途，放射性核素偶联药物可分为诊断用和治疗用2大类。国际药物监管相关机构如国际人用药品注册技术协调会（ICH）、美国食品药品监督管理局（FDA）、欧洲药品管理局（EMA）以及中国国家药品监督管理局（NMPA）和国际原子能机构（IAEA）等分别制定了相应的指导原则以规范其非临床安全性评价过程，综合分析各指导原则的异同；同时解读2018—2024年FDA批准的治疗用RDCs非临床安全性评价的要点和异同，为开展治疗用RDCs的非临床安全性研究提供参考。

Radionuclide drug conjugates (RDCs) are compounds that link radioactive isotopes with drug molecules, RDCs are designed to effectively kill tumor cells in vivo by harnessing their unique internal radiation exposure. Additionally, they exhibit abscopal effects and bystander effects, demonstrating significant potential for treating disseminated tumors. According to the purpose of the linked isotopes, radionuclide drug conjugates can be classified into diagnostic and therapeutic categories. International drug related regulatory agencies such as FDA, EMA, NMPA, and IAEA have issued corresponding guidelines to standardize the non-clinical safety evaluation process. This review comprehensively analyzes the similarities and differences among these guidelines and interprets the key points and differences in non-clinical safety evaluations on radiotherapeutic drugs approved by the FDA from 2018 to 2024, providing a reference for conducting non-clinical safety evaluations on therapeutic radionuclide drug conjugates.

R979.1