He Haiqi, Deng Xin, Wang Zhijie, Chen Jianjun
Guangdong Provincial Key Laboratory of New Drug Screening, NMPA Key Laboratory for Research and Evaluation of Drug Metabolism, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China.
Guangzhou Municipal and Guangdong Provincial Key Laboratory of Molecular Target & Clinic Al Pharmacology, The NMPA and State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences and the Fifth Affiliated Hospital, Guangzhou Medical University, Guangzhou, 511436, China.
Eur J Med Chem. 2025 Feb 15;284:117204. doi: 10.1016/j.ejmech.2024.117204. Epub 2024 Dec 24.
Peptide-drug conjugates (PDCs) are emerging therapeutic agents composed of peptides, linkers, and payloads, which possess favorable targeting capability and can deliver enough payloads to the tumor sites with minimized impact on healthy tissues. However, only a few PDCs have been approved for clinical use so far. To advance the research on PDCs, this review summarizes the approved PDCs, and PDCs in clinical and preclinical stages based on the payload types. Additionally, the biological activity and pharmacokinetic properties of preclinical PDCs are detailedly described. Lastly, the challenges and future development directions of PDCs are discussed. This review aims to inspire insights into the development of PDCs for cancer treatment.
肽-药物偶联物（PDC）是由肽、连接子和有效载荷组成的新兴治疗剂，具有良好的靶向能力，能够在对健康组织影响最小的情况下将足够的有效载荷递送至肿瘤部位。然而，迄今为止只有少数PDC被批准用于临床。为了推进PDC的研究，本综述根据有效载荷类型总结了已批准的PDC以及处于临床和临床前阶段的PDC。此外，还详细描述了临床前PDC的生物活性和药代动力学性质。最后，讨论了PDC面临的挑战和未来发展方向。本综述旨在激发对用于癌症治疗的PDC开发的见解。
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