Analytical Sciences, Biopharmaceutical Development, AstraZeneca, Gaithersburg, MD, USA.
Biologics Operations, AstraZeneca, Frederick, MD, USA.
MAbs. 2020 Jan-Dec;12(1):1738691. doi: 10.1080/19420862.2020.1738691.
When two therapeutic agents are combined in a single formulation, i.e., coformulated, the quality and safety of the individual agents must be preserved. Here we describe an approach to evaluate the quality attributes of two individual monoclonal antibodies (mAbs), designated mAb-A and mAb-B, in coformulation. The mAbs were fractionated from heat-stressed coformulated drug product (DP) by hydrophobic interaction chromatography. Each purified mAb fraction was then compared with mAb-A and mAb-B in their individual formulations from the same drug substance sources used to make the coformulated DP lot, which was subjected to the same stress conditions. Product variants were evaluated and compared by using several analytical tests, including high-performance size exclusion chromatography (HPSEC), reducing and nonreducing gel electrophoresis, ion-exchange chromatography, capillary isoelectric focusing, and peptide mapping with mass spectrometry. Intermolecular interactions in coformulated and photostressed DPs were studied by evaluating aggregates fractionated from coformulated DP by HPSEC. Aggregate fractions of coformulated DP contained dimers, but not coaggregates, of mAb-A or mAb-B. Moreover, extensive assays for higher-order structure and biological interactions confirmed that there was no interaction between the two mAb molecules in the coformulation. These results demonstrate that the two coformulated therapeutic mAbs had the same quality attributes as the individually formulated mAb-A and mAb-B, no new quality attributes were formed, and no physicochemical, intermolecular, or biological interactions occurred between the two components. The approach described here can be used to monitor the product quality of other coformulated antibodies.
当两种治疗剂在单一配方中组合使用时,即共配制,必须保持各治疗剂的质量和安全性。在此,我们描述了一种评估两种单克隆抗体(mAb),即 mAb-A 和 mAb-B 在共配制中的质量属性的方法。将 mAb 从受热共配制药物产品(DP)中通过疏水相互作用色谱法进行分离。然后,将每个纯化的 mAb 级分与来自同一药物物质来源的 mAb-A 和 mAb-B 的单独配方中的级分进行比较,这些 mAb 是用于制备共配制 DP 批次的物质,且经历了相同的应激条件。通过使用几种分析测试,包括高效尺寸排阻色谱(HPSEC)、还原和非还原凝胶电泳、离子交换色谱、毛细管等电聚焦和肽图谱与质谱联用,对产品变体进行评估和比较。通过评估 HPSEC 从共配制 DP 中分离的聚集体来研究共配制和光应激 DP 中的分子间相互作用。共配制 DP 的聚集体级分含有 mAb-A 或 mAb-B 的二聚体,但没有共聚集体。此外,对高级结构和生物学相互作用的广泛检测证实,两种 mAb 分子在共配制中没有相互作用。这些结果表明,两种共配制的治疗性 mAb 具有与单独配制的 mAb-A 和 mAb-B 相同的质量属性,没有形成新的质量属性,并且两种成分之间没有发生物理化学、分子间或生物学相互作用。这里描述的方法可用于监测其他共配制抗体的产品质量。