School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, China.
WuXi Biologics Co, Ltd., Shanghai 200131, China.
Bioconjug Chem. 2021 Aug 18;32(8):1525-1534. doi: 10.1021/acs.bioconjchem.1c00213. Epub 2021 Jun 9.
Antibody-drug conjugates (ADCs) have attracted great attention in recent years in the wake of an accelerated FDA approval rate and several large-scale acquisitions. To date, there are ten ADC drugs on the market and more than 70 in various stages of clinical trials. Yet, due to the complicated nature of ADC molecules, considerations need to cover many aspects for the success of ADCs, including target specificity, linker-payload stability, tumor permeability, and clearance rate. This topical review summarizes and discusses current methods used to increase stability and homogeneity of ADCs of cysteine conjugation. We believe that they will lead to improvement of efficacy and pharmacokinetics (PK) of ADC drugs.
抗体偶联药物（ADCs）在 FDA 批准率加快和几宗大型收购的推动下，近年来受到了极大关注。迄今为止，市面上有十种 ADC 药物，还有七十多种处于不同临床试验阶段。然而，由于 ADC 分子的复杂性，需要考虑许多方面才能使 ADC 成功，包括靶标特异性、连接子-载药稳定性、肿瘤通透性和清除率。本专题综述总结并讨论了目前用于提高半胱氨酸偶联 ADC 稳定性和均一性的方法。我们相信，这些方法将提高 ADC 药物的疗效和药代动力学（PK）。
