Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK.
Chem Soc Rev. 2019 Aug 12;48(16):4361-4374. doi: 10.1039/c8cs00676h.
Antibody-Drug Conjugates (ADCs) are now established as a major class of therapeutics for the clinical treatment of cancer. The properties of the linker between the antibody and the payload are proven to be critical to the success of an ADC. Although ADC linkers can be 'non-cleavable', the vast majority of ADCs in clinical development have specific release mechanisms to allow controlled linker cleavage at the target site and are thus termed 'cleavable'. In recent years, the development of new methods of drug release from ADCs has continued in parallel to the deepening understanding of the biological processes underlying the mechanisms of action of pre-existing technologies. This review summarises the advances in the field of cleavable linker technologies for ADCs.
抗体药物偶联物（ADCs）现已成为癌症临床治疗的一类主要治疗药物。抗体与有效载荷之间的连接物的性质被证明对 ADC 的成功至关重要。尽管 ADC 接头可以是非可裂解的，但在临床开发中的绝大多数 ADC 都具有特定的释放机制，可在靶部位允许控制的接头裂解，因此被称为“可裂解的”。近年来，随着对现有技术作用机制的生物学过程的深入了解，从 ADC 中释放药物的新方法的开发也在不断发展。本文综述了 ADC 可裂解连接子技术领域的进展。
