抗体药物偶联物（ADC）是有前途的癌症治疗药物，与单独的小细胞毒素分子相比，毒性最小，并已显示出克服肿瘤耐药性和预防癌症复发的证据。ADC具有改变癌症化学治疗治疗范例的潜力。目前，美国FDA已批准13种ADC用于治疗各种固体肿瘤和血液恶性肿瘤。该综述涵盖ADC的三个结构组成部分-抗体、链接物和细胞毒素荷载物-以及它们各自的结构、化学、作用机制和对ADC活性的影响。它全面阐述了链接物对ADC功效、稳定性和毒性的结构作用、不同类型的链接物和各种偶联技术。该文章概述了用于定性和定量分析ADC的各种分析技术。此外，还概述了ADC的当前挑战，例如异质性、旁观者效应、蛋白聚集、内化效率低或进入肿瘤细胞能力差、治疗指数狭窄、耐药性等的最新进展以及未来发展更有前途的下一代ADC的机遇。 © 2023. 韩国药学学会。

Antibody drug conjugates (ADCs) are promising cancer therapeutics with minimal toxicity as compared to small cytotoxic molecules alone and have shown the evidence to overcome resistance against tumor and prevent relapse of cancer. The ADC has a potential to change the paradigm of cancer chemotherapeutic treatment. At present, 13 ADCs have been approved by USFDA for the treatment of various types of solid tumor and haematological malignancies. This review covers the three structural components of an ADC-antibody, linker, and cytotoxic payload-along with their respective structure, chemistry, mechanism of action, and influence on the activity of ADCs. It covers comprehensive insight on structural role of linker towards efficacy, stability & toxicity of ADCs, different types of linkers & various conjugation techniques. A brief overview of various analytical techniques used for the qualitative and quantitative analysis of ADC is summarized. The current challenges of ADCs, such as heterogeneity, bystander effect, protein aggregation, inefficient internalization or poor penetration into tumor cells, narrow therapeutic index, emergence of resistance, etc., are outlined along with recent advances and future opportunities for the development of more promising next-generation ADCs.© 2023. The Pharmaceutical Society of Korea.