Late Stage Pharmaceutical and Processing Development, Genentech, Inc., South San Francisco, CA, USA.
MAbs. 2011 Mar-Apr;3(2):161-72. doi: 10.4161/mabs.3.2.14960. Epub 2011 Mar 1.
Antibody-drug conjugates (ADCs), formed through the chemical linkage of a potent small molecule cytotoxin (drug) to a monoclonal antibody, have more complex and heterogeneous structures than the corresponding antibodies. This review describes the analytical methods that have been used in their physicochemical characterization. The selection of the most appropriate methods for a specific ADC is heavily dependent on the properties of the linker, the drug, and the choice of attachment sites (lysines, inter-chain cysteines, Fc glycans). Improvements in analytical techniques such as protein mass spectrometry and capillary electrophoresis have significantly increased the quality of information that can be obtained for use in product and process characterization, and for routine lot release and stability testing.
抗体药物偶联物 (ADCs) 是通过将有效的小分子细胞毒素（药物）化学连接到单克隆抗体上形成的，其结构比相应的抗体更为复杂和多样。本综述描述了用于其理化特性分析的方法。选择最适合特定 ADC 的方法在很大程度上取决于连接子、药物以及连接部位（赖氨酸、链间半胱氨酸、Fc 聚糖）的选择。蛋白质质谱和毛细管电泳等分析技术的改进极大地提高了可用于产品和工艺特性分析以及常规批次放行和稳定性测试的信息质量。
