Institute of Pharmaceutical Science, School of Cancer and Pharmaceutical Sciences, King's College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 9NH, UK.
Institute of Pharmaceutical Science, School of Cancer and Pharmaceutical Sciences, King's College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 9NH, UK.
Drug Discov Today. 2022 Jan;27(1):354-361. doi: 10.1016/j.drudis.2021.09.015. Epub 2021 Sep 28.
In antibody-drug conjugates (ADCs), monoclonal antibodies (mAbs) act as carriers for a cytotoxic payload providing the therapy with targeted action against cells expressing a target cell surface antigen. An appropriate choice of mAb is crucial to developing a successful ADC for clinical development. However, problems such as immunogenicity, poor pharmacokinetic (PK) and pharmacodynamic (PD) profiles and variable drug-antibody ratios (DARs) plague ADCs. In this review, we detail recent mAb-based innovations and factors that should be considered to overcome these problems to achieve a new generation of more effective ADC therapeutics.
在抗体药物偶联物 (ADC) 中，单克隆抗体 (mAb) 作为细胞毒有效载荷的载体，为表达靶细胞表面抗原的细胞提供靶向作用的治疗。选择合适的 mAb 对于开发用于临床开发的成功 ADC 至关重要。然而，免疫原性、较差的药代动力学 (PK) 和药效学 (PD) 特征以及可变的药物抗体比 (DAR) 等问题困扰着 ADC。在这篇综述中，我们详细介绍了最近基于 mAb 的创新和应考虑克服这些问题以实现新一代更有效的 ADC 治疗的因素。
