Advances and prospects of nitroimidazole radiopharmaceuticals targeting tumor hypoxia

WANG Chengdong; DU Jin; RUAN Qing; ZHANG Junbo nbsp

doi:10.19732/j.cnki.2096-6210.2024.04.002

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Advances and prospects of nitroimidazole radiopharmaceuticals targeting tumor hypoxia

更新时间：2025-12-15

- Advances and prospects of nitroimidazole radiopharmaceuticals targeting tumor hypoxia
- Vol. 33, Issue 4, Pages: 342-354(2024)
- 作者机构：
  
  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
- 作者简介：
- 基金信息：
- DOI：10.19732/j.cnki.2096-6210.2024.04.002
  CLC：
- Published Online：11 September 2024，
  
  Published：11 September 2024
- 稿件说明：
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王成栋,杜进,阮晴,等. 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[J]. 肿瘤影像学, 2024, 33(4): 342-354 https://doi.

org/10.19732/j.cnki.2096-6210.2024.04.002
王成栋,杜进,阮晴,等. 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[J]. 肿瘤影像学, 2024, 33(4): 342-354 https://doi. DOI： 10.19732/j.cnki.2096-6210.2024.04.002.

org/10.19732/j.cnki.2096-6210.2024.04.002 DOI：

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。

Abstract

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.

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