放射性核素偶聯(lián)藥物（RDCs）是一類將放射性同位素與藥物分子結(jié)合的化合物，該類藥物在體內(nèi)起效時(shí)會(huì)借助其獨(dú)有的內(nèi)照射有效殺傷腫瘤細(xì)胞，且具有遠(yuǎn)端效應(yīng)以及旁觀者效應(yīng)，在治療擴(kuò)散性腫瘤時(shí)具有較大應(yīng)用潛力。根據(jù)所結(jié)合的核素用途，放射性核素偶聯(lián)藥物可分為診斷用和治療用2大類。國(guó)際藥物監(jiān)管相關(guān)機(jī)構(gòu)如國(guó)際人用藥品注冊(cè)技術(shù)協(xié)調(diào)會(huì)（ICH）、美國(guó)食品藥品監(jiān)督管理局（FDA）、歐洲藥品管理局（EMA）以及中國(guó)國(guó)家藥品監(jiān)督管理局（NMPA）和國(guó)際原子能機(jī)構(gòu)（IAEA）等分別制定了相應(yīng)的指導(dǎo)原則以規(guī)范其非臨床安全性評(píng)價(jià)過(guò)程，綜合分析各指導(dǎo)原則的異同；同時(shí)解讀2018—2024年FDA批準(zhǔn)的治療用RDCs非臨床安全性評(píng)價(jià)的要點(diǎn)和異同，為開(kāi)展治療用RDCs的非臨床安全性研究提供參考。

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