多肽偶联药物:下一代靶向治疗的方向

Polypeptide-drug conjugates: a new direction in targeted therapy

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DOI 10.12208/j.imrf.20250039
刊名
International Medical Research Frontier
年,卷(期) 2025, 9(4)
作者
作者单位

中国药科大学 江苏南京

摘要
多肽偶联药物(PDCs)作为新一代靶向治疗平台,通过共价键将具有靶向功能的肽段、细胞毒性载荷和连接子结合,构成了一个精准的药物递送系统。与抗体偶联药物(ADCs)相比,PDCs凭借其更小的分子尺寸、组织穿透性、合成简便性、生产成本及设计灵活性方面展现出显著优势。然而,PDCs的临床转化仍面临诸多挑战,主要包括多肽固有的代谢不稳定性、血液循环半衰期短、口服生物利用度低等问题。文章就PDCs的组成、临床应用进展、提高治疗效果的策略进行了综述,旨在为开发效果更佳的PDCs类抗肿瘤药物提供理论依据和研究思路。
Abstract
Peptide-drug conjugates (PDCs), as a new generation of targeted therapeutic platforms, form a precise drug delivery system by covalently linking targeting peptides, cytotoxic payloads, and linkers. Compared to antibody-drug conjugates (ADCs), PDCs demonstrate significant advantages in terms of smaller molecular size, tissue penetration, ease of synthesis, production cost, and design flexibility. However, the clinical translation of PDCs still faces several challenges, including inherent metabolic instability of peptides, short half-life in systemic circulation, and low oral bioavailability. This article reviews the composition of PDCs, progress in clinical applications, and strategies to enhance therapeutic efficacy, aiming to provide a theoretical basis and research insights for the development of more effective PDC-based anticancer drugs.
关键词
多肽偶联药物;靶向治疗;连接子
KeyWord
Peptide-drug conjugates; Targeted therapy; Linkers
基金项目
页码 15-19
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吴君臣, 徐翀, 姚彧远, 张薛龙. 多肽偶联药物:下一代靶向治疗的方向 [J]. 国际医药研究前沿. 2025; 9; (4). 15 - 19.

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