<sup>177</sup>Lu标记多肽类放射性药物研究进展

徐千龙; 李凤林; 冯荷娟; 史豪杰; 唐显

doi:10.11889/j.1000-3436.2025-0082

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¹⁷⁷Lu标记多肽类放射性药物研究进展

综述 | 更新时间：2026-02-06

- ¹⁷⁷Lu标记多肽类放射性药物研究进展
- The development of ¹⁷⁷Lu labelled peptides
- 辐射研究与辐射工艺学报 2026年44卷第1期页码：10102
- 作者机构：
  
  1.中国原子能科学研究院北京 102413
  2.重庆市万州粮油质量监督检验站重庆 404001
- 作者简介：
  
  徐千龙，男，2000年3月出生，2022年7月于大连理工大学获学士学位，现为中国原子能科学研究院在读硕士生，研究方向为放射性药物
  李凤林，研究员，E-mail: lifenglin@ciae.ac.cn
  唐显，高级工程师，E-mail: tangxian@ciae.ac.cn
- 基金信息：
  
  中国原子能科学研究院院长基金项目(YZ222501001204)
- DOI：10.11889/j.1000-3436.2025-0082
  中图分类号： R817.9
- 收稿：2025-09-10，
  
  修回：2026-01-04，
  
  录用：2026-01-04，
  
  纸质出版：2026-02-20
- 稿件说明：
移动端阅览
徐千龙, 李凤林, 冯荷娟, 等. ¹⁷⁷Lu标记多肽类放射性药物研究进展[J]. 辐射研究与辐射工艺学报, 2026, 44(1): 010102.

XU Qianlong, LI Fenglin, FENG Hejuan, et al. The development of ¹⁷⁷Lu labelled peptides[J]. Journal of Radiation Research and Radiation Processing, 2026, 44(1): 010102.
徐千龙, 李凤林, 冯荷娟, 等. ¹⁷⁷Lu标记多肽类放射性药物研究进展[J]. 辐射研究与辐射工艺学报, 2026, 44(1): 010102. DOI： 10.11889/j.1000-3436.2025-0082. CSTR： 32195.14.j.JRRRP.1000-3436.2025-0082.

XU Qianlong, LI Fenglin, FENG Hejuan, et al. The development of ¹⁷⁷Lu labelled peptides[J]. Journal of Radiation Research and Radiation Processing, 2026, 44(1): 010102. DOI： 10.11889/j.1000-3436.2025-0082. CSTR： 32195.14.j.JRRRP.1000-3436.2025-0082.

摘要

177

Lu具有优良的物理特性，而多肽具有分子量小、生物相容性好以及合成简便、易于修饰的优良性质，使得以

177

Lu-DOTATATE为代表的

177

Lu标记多肽类放射性药物在肿瘤治疗研究中展示出良好的疗效，引发了科研人员对此类药物的研究热潮。多聚化、双靶向设计以及血液半衰期延长修饰等策略的组合应用，是提高靶向多肽肿瘤滞留的关键技术路径。本文对近年来研究较多的

177

Lu标记多肽类放射性药物的靶点、多肽分子的修饰策略、

177

Lu标记多肽类放射性药物的临床前及临床研究数据等进行综述，并对该类药物的优缺点、发展趋势等进行了对比分析。结果表明，该类药物拥有较好的安全性和治疗效果，具有广阔的应用前景。

Abstract

177

Lu possesses excellent physical properties

while peptides exhibit fine qualities such as small molecular weight

good biocompatibility

simple synthesis

and convenient modification. This combination makes

177

Lu-labeled peptide radiopharmaceuticals

represented by

177

Lu-DOTATATE

demonstrate good efficacy in tumor treatment research

sparking a surge of interest in this type of drug among researchers. The combined application of strategies such as multimerization

dual-targeting design

and modification to prolong blood half-life are key technological paths for improving the tumor retention of targeted peptides. This article reviews the targets

modification strategies of peptide molecules

preclinical and clinical research data of

177

Lu-labeled peptide radiopharmaceuticals that have been extensively studied in recent years. It also conducts a comparative analysis of the advantages and disadvantages

as well as the development trends of this type of drug. The results indicate that this type of drug possesses good safety and therapeutic effects

with broad application prospects.

关键词

Keywords

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177Lu标记多肽类放射性药物研究进展

The development of 177Lu labelled peptides

DOI：10.11889/j.1000-3436.2025-0082

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¹⁷⁷Lu标记多肽类放射性药物研究进展

The development of ¹⁷⁷Lu labelled peptides