靶向肿瘤乏氧的硝基咪唑类放射性药物的研究现状及展望  

Advances and prospects of nitroimidazole radiopharmaceuticals targeting tumor hypoxia

作　　者：王成栋 杜进[2,4,5] 阮晴 张俊波 WANG Chengdong;DU Jin;RUAN Qing;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,China;Department of Nuclear Technology and Application,China Institute of Atomic Energy,Beijing 102413,China;Department of Nuclear Medicine,The First Affiliated Hospital of Dalian Medical University,Dalian 116300,Liaoning Province,China;China Isotope&Radiation Corporation,Beijing 100089,China;CAEA Center of Excellence on Nuclear Technology Application for Engineering and Industrialization of Radiopharmaceuticals,Beijing 102413,China;Key Laboratory of Beam Technology of the Ministry of Education,School of Physics and Astronomy,Beijing Normal University,Beijing 100875,China)

机构地区：[1]放射性药物教育部重点实验室,国家药监局放射性药物研究与评价重点实验室,北京师范大学化学学院,北京100875 [2]中国原子能科学研究院核技术及综合所,北京102413 [3]大连医科大学附属第一医院核医学科,辽宁大连116300 [4]中国同辐股份有限公司,北京100089 [5]国家原子能机构核技术(放射性药物工程转化)研发中心,北京102413 [6]射线束技术教育部重点实验室,北京师范大学物理与天文学院,北京100875

出　　处：《肿瘤影像学》2024年第4期342-354,共13页Oncoradiology

基　　金：国家自然科学基金(22076013,22276015);北京市自然科学基金(2232010);北京市科技新星交叉合作课题(20230484470);中国博士后科学基金(2022M720464)。

摘　　要：乏氧常见于大多数实体肿瘤,并与肿瘤进展、转移和放化疗耐药性相关。正电子发射体层成像(positron emission tomography,PET)和单光子发射计算机体层成像(single-photon emission computed tomography,SPECT)技术使用靶向乏氧放射性药物可以实现肿瘤乏氧的无创可视化监测。硝基咪唑能够选择性地保留在乏氧细胞内部,因而成为靶向乏氧放射性药物的重要药效团。近年来含硝基咪唑的靶向乏氧放射性药物已被用于检测肿瘤乏氧。本文总结了近10年来硝基咪唑类肿瘤乏氧放射性药物的研究现状并对其未来发展趋势予以展望。Hypoxia,a common status of most solid tumors,is associated with tumor progression,metastasis,radiotherapy and chemotherapy resistance.Positron emission tomography(PET)and single-photon emission computed tomography(SPECT)using hypoxic-targeting radiopharmaceuticals have been applied to non-invasive monitoring of tumor hypoxia.Nitroimidazole,which could be selectively trapped within hypoxia cells,has become an important pharmacophore for targeting hypoxia.Recently,hypoxic-targeting radiopharmaceuticals containing nitroimidazole have been developed for detecting tumor hypoxia.In this review,the progress of hypoxic-targeting radiopharmaceuticals containing nitroimidazole in recent ten years was introduced and the future development direction was also prospected.

关 键 词：肿瘤乏氧 硝基咪唑 放射性药物 

分 类 号：R445.5[医药卫生—影像医学与核医学]