Peng Wenjing, Yan Yuetian, Cotham Victoria C, Heindel Andrew, Wang Shunhai, Li Ning
Analytical Chemistry Group, Regeneron Pharmaceuticals, Tarrytown, NY, 10591, USA.
Sci Rep. 2025 Jul 31;15(1):28042. doi: 10.1038/s41598-025-13986-1.
Co-formulation of two or more therapeutic monoclonal antibodies (mAbs) into one final drug product has gained significant popularity recently due to its numerous advantages, including enhanced efficacy, reduced overall adverse events, and improved patient convenience and compliance. However, the increased heterogeneity of mAb cocktails introduces additional challenges for both formulation development and analytical characterization. Specifically, the identification and quantitation of various dimer species in mAb cocktails is particularly challenging due to their low abundances and highly similar biophysical properties. Traditional analytical tools used for dimer analysis in mAb monotherapy products often lack the specificity needed to distinguish between heterodimers and homodimers. In this study, we report the development and evaluation of a size-exclusion chromatography method coupled to online native mass spectrometry (nSEC-MS) for analyzing dimers in mAb cocktails. Various sample treatment strategies, such as deglycosylation and immunodepletion, were developed to facilitate the differentiation and quantitation of dimer species in two- and three-mAb cocktails. Additionally, key parameters in SEC separation (e.g., flow rate) and MS data acquisition (e.g., resolution settings) were explored to improve method throughput and sensitivity. Together, this optimized nSEC-MS method and associated analytical strategies were demonstrated to be highly effective in identification and quantitation of various hetero- and homodimer species and can be widely applied to support the development of mAb cocktail products.
将两种或更多种治疗性单克隆抗体(mAb)共同配制到一种最终药物产品中,由于其诸多优点,包括增强疗效、减少总体不良事件以及提高患者便利性和依从性,近年来已变得非常流行。然而,mAb混合物中增加的异质性给制剂开发和分析表征都带来了额外挑战。具体而言,由于mAb混合物中各种二聚体种类的丰度低且生物物理性质高度相似,对其进行鉴定和定量尤其具有挑战性。用于mAb单药治疗产品中二聚体分析的传统分析工具通常缺乏区分异二聚体和同二聚体所需的特异性。在本研究中,我们报告了一种尺寸排阻色谱法与在线天然质谱(nSEC-MS)联用的方法的开发和评估,用于分析mAb混合物中的二聚体。开发了各种样品处理策略,如去糖基化和免疫去除,以促进对双mAb和三mAb混合物中二聚体种类的区分和定量。此外,还探索了SEC分离中的关键参数(如流速)和MS数据采集(如分辨率设置),以提高方法通量和灵敏度。总之,这种优化的nSEC-MS方法和相关分析策略在鉴定和定量各种异二聚体和同二聚体种类方面被证明是非常有效的,并且可广泛应用于支持mAb混合物产品的开发。