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Strategies and research advances in enhancing the therapeutic efficacy of peptide-drug conjugates for tumor treatment
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Xue-dan WANG1, Wen-jing GAO2, Mao-long CHEN1, Zhi-jian HAN3, *, Ya-ping MA4, Yu-en WANG4, Jian-ping MA1, *
Acta Pharmaceutica Sinica | 2025, 60(7) : 2072 - 2083
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Acta Pharmaceutica Sinica | 2025, 60(7): 2072-2083
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Strategies and research advances in enhancing the therapeutic efficacy of peptide-drug conjugates for tumor treatment
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Xue-dan WANG1, Wen-jing GAO2, Mao-long CHEN1, Zhi-jian HAN3, *, Ya-ping MA4, Yu-en WANG4, Jian-ping MA1, *
Affiliations
  • 1School of Life Science and Engineering, Lanzhou University of Technology, Lanzhou 730000, China
  • 2Lanzhou Jishi Pharmaceutical Co., Ltd., Lanzhou 730000, China
  • 3Cancer Center, the Second Hospital of Lanzhou University, Lanzhou 730000, China
  • 4Shenzhen Shenchuang Biopharmaceutical Co., Ltd., Shenzhen 518000, China
Published: 2025-07-12 doi: 10.16438/j.0513-4870.2025-0159
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Cancer therapeutic drugs include traditional chemotherapy drugs, targeted therapy drugs, monoclonal antibodies, as well as novel antibody-drug conjugates (ADCs) and peptide-drug conjugates (PDCs). PDCs have demonstrated significant clinical advantages in cancer treatment, but they still face limitations such as poor stability and insufficient targeting specificity. In recent years, the application of multivalent targeting peptide strategies and dual targeting peptide strategies has significantly improved the targeting precision of PDCs. Meanwhile, molecular engineering approaches such as peptide cyclization, unnatural amino acid substitution, and fatty acid chain modification have effectively enhanced the in vivo stability of PDCs. These innovative strategies have markedly strengthened the pharmacological activity of PDCs and their therapeutic efficacy in tumors. Based on the structural characteristics and research progress of PDCs, this article systematically reviews the latest strategies for improving the targeting ability, stability, and cell membrane penetration efficiency of PDCs, aiming to provide a theoretical foundation and research insights for the development of PDC-based anticancer drugs with superior pharmacodynamic properties.

peptide-drug conjugate  /  targeting specificity  /  stability  /  tumor  /  therapeutic efficacy
王雪丹, 高文静, 陈卯龙, 韩志坚, 马亚平, 王宇恩, 马建苹. 多肽药物偶联物及其提高肿瘤疗效的改进策略和研究进展. 药学学报, 2025 , 60 (7) : 2072 -2083 . DOI: 10.16438/j.0513-4870.2025-0159
Xue-dan WANG, Wen-jing GAO, Mao-long CHEN, Zhi-jian HAN, Ya-ping MA, Yu-en WANG, Jian-ping MA. Strategies and research advances in enhancing the therapeutic efficacy of peptide-drug conjugates for tumor treatment[J]. Acta Pharmaceutica Sinica, 2025 , 60 (7) : 2072 -2083 . DOI: 10.16438/j.0513-4870.2025-0159
Year 2025 volume 60 Issue 7
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137
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Article Info
doi: 10.16438/j.0513-4870.2025-0159
  • Receive Date:2025-02-19
  • Online Date:2026-09-20
  • Published:2025-07-12
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History
  • Received:2025-02-19
  • Revised:2025-04-14
Affiliations
    1School of Life Science and Engineering, Lanzhou University of Technology, Lanzhou 730000, China
    2Lanzhou Jishi Pharmaceutical Co., Ltd., Lanzhou 730000, China
    3Cancer Center, the Second Hospital of Lanzhou University, Lanzhou 730000, China
    4Shenzhen Shenchuang Biopharmaceutical Co., Ltd., Shenzhen 518000, China
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表12种不同金属材料的力学参数
科
Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)
属
Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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