抗体药物偶联物（ADC）将单克隆抗体的靶向性与细胞毒性药物的杀伤力相结合，已成为肿瘤治疗领域的重大突破之一。历经多轮技术迭代，ADC在疗效与安全性上实现了跨越式提升，但设计优化与制备质控的复杂性仍制约其产业化转化与临床应用。系统梳理ADC技术迭代历程，从设计阶段的多环节协同控制、制备过程的质量管控2大核心维度，剖析靶点匹配、偶联工艺、质控标准等关键技术要点，深入探讨当前ADC研发面临的实体瘤穿透瓶颈、耐药性及产业化成本等核心挑战，并对人工智能（AI）辅助设计、新型偶联技术及个性化ADC的发展前景进行展望，以期为ADC的研发提供全面的技术参考与前瞻性视角，为ADC药物的高效研发与规范化生产提供参考。

Antibody-drug conjugates (ADCs), which combine the targeting specificity of monoclonal antibodies with the potent lethality of cytotoxic drugs, have emerged as a major breakthrough in cancer therapy. Through generations of technological evolution, ADCs have achieved significant improvements in both efficacy and safety. However, the inherent complexities in design optimization, manufacturing, and quality control continue to pose challenges for their broader industrial translation and clinical application. This review provides a systematic review of the evolution of ADC technology. It analyzes critical technical aspects from two core perspectives: The coordinated control across multiple design stages and the quality management throughout the manufacturing process. Key elements examined include target selection, conjugation strategies, and established quality control standards. The article further delves into the central challenges currently facing ADC development, such as limited penetration into solid tumors, the emergence of drug resistance, and the high costs associated with industrial-scale production. Finally, it offers a forward-looking perspective on emerging trends, including AI-aided rational design, novel conjugation platforms, and the potential for personalized ADC therapies. This comprehensive analysis aims to serve as both a technical reference and a strategic outlook, providing insights to facilitate the efficient development and standardized production of next-generation ADC therapeutics.

R979.1

中国博士后科学基金面上资助项目（2021M702453）；天津市科技计划项目（25YDTPJC00740）