基于松散相互作用层QCM-D度量的单克隆抗体自关联及溶液行为预测

IF 4.5 2区 医学 Q2 MEDICINE, RESEARCH & EXPERIMENTAL
Molecular Pharmaceutics Pub Date : 2025-04-07 Epub Date: 2024-11-29 DOI:10.1021/acs.molpharmaceut.4c00656
Yusra Rahman, Siddhanth Hejmady, Reza Nejadnik
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引用次数: 0

摘要

尽管单克隆抗体(mAb)的可用性和成功度不断提高,但由于自身关联和溶液行为不佳,早期鉴定具有理想可发展性属性的候选分子仍然具有挑战性。在单克隆抗体的开发过程中,利用现有的实验方法测量这些现象是很复杂的。石英晶体微天平耗散监测(QCM-D)检测到分子不可逆吸附层上的松散相互作用层,提供单克隆抗体相互作用的信息。这项工作旨在探索该层的特征是否可以用作可靠的自关联度量。QCM-D实验显示,omalizumab的大频移(Δf)与松散相互作用层有关,而tocilizumab的小频移或无频移。因此,与托珠单抗相比,omalizumab的黏度在高浓度下呈指数增长。对8种具有不同自关联行为的单抗的测试显示,最常用的自关联度量,即扩散相互作用参数(kD-DLS)与Δf之间存在很强的秩序相关性,表明Δf具有预测单抗溶液行为的潜力。与敏感的kD-DLS相比,该研究还强调了该度量对杂质和温度变化的鲁棒性。总的来说,我们证明了松散相互作用层提供了关于单克隆抗体自我关联的有价值的信息,预测了治疗开发中的胶体稳定性和溶液行为。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Prediction of Self-Association and Solution Behavior of Monoclonal Antibodies Using the QCM-D Metric of Loosely Interacting Layer.

Despite the increasing availability and success of monoclonal antibodies (mAb), early identification of candidate molecules with desirable developability attributes remains challenging due to self-association and poor solution behavior. Measuring these phenomena experimentally using the available methods is complicated in mAbs development. Quartz crystal microbalance with dissipation monitoring (QCM-D) detects a loosely interacting layer on top of the irreversibly adsorbed layer of molecules, providing information about the mAbs interaction. This work aimed to explore whether the characteristics of this layer can be used as a reliable self-association metric. QCM-D experiments showed a large frequency shift (Δf) associated with loosely interacting layers for omalizumab but a small or absent layer for tocilizumab. Accordingly, the viscosity of omalizumab increased exponentially at high concentrations compared to tocilizumab. Testing eight mAbs with different self-association behaviors revealed a strong rank order correlation between the mostly used metric of self-association, i.e., diffusion interaction parameter (kD-DLS), and Δf, indicating Δf's potential for predicting mAb solution behavior. The study also highlighted the robustness of the metric to impurities and temperature variations compared to the sensitive kD-DLS. Overall, we demonstrate that the loosely interacting layer provides valuable information about mAb self-association, predicting the colloidal stability and solution behavior in therapeutic development.

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来源期刊
Molecular Pharmaceutics
Molecular Pharmaceutics 医学-药学
CiteScore
8.00
自引率
6.10%
发文量
391
审稿时长
2 months
期刊介绍: Molecular Pharmaceutics publishes the results of original research that contributes significantly to the molecular mechanistic understanding of drug delivery and drug delivery systems. The journal encourages contributions describing research at the interface of drug discovery and drug development. Scientific areas within the scope of the journal include physical and pharmaceutical chemistry, biochemistry and biophysics, molecular and cellular biology, and polymer and materials science as they relate to drug and drug delivery system efficacy. Mechanistic Drug Delivery and Drug Targeting research on modulating activity and efficacy of a drug or drug product is within the scope of Molecular Pharmaceutics. Theoretical and experimental peer-reviewed research articles, communications, reviews, and perspectives are welcomed.
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