An Instrument to Determine Protein Stability for Biologics Formulations Testing

简介(申请人提供)：蛋白质疗法是生物技术和制药行业中增长最快的领域，年销售额超过700亿美元。蛋白质疗法包括单抗、重组蛋白、嵌合蛋白和其他蛋白质受体结构。蛋白质作为药物开发的一个主要障碍是其安全和稳定的形式。在发育过程中，最大限度地提高其稳定性和消除蛋白质聚集的缓冲液、配体和赋形剂条件的确定是至关重要的，通常需要对数百种条件进行评估。由于缺乏能够准确测量蛋白质稳定性/聚集矩阵的全自动仪器，这项耗时的任务变得更加复杂。这项提议的目标是开发一种全自动的蛋白质化学变性荧光仪器，旨在测量多维蛋白质稳定性和聚集基质。与目前任何其他可用的仪器不同，该仪器将能够自动准备和分析多达96条蛋白质变性曲线-足以完成新生物的整个配方研究。在这台仪器中，用户只需要提供蛋白质和原料药解决方案。该仪器将自动准备所有溶液，执行测量，分析数据，并将结果呈现给研究人员。 公共卫生相关性：该仪器将极大地加速蛋白质疗法的发展，并找到一个重要的市场。此外，它还将为研究蛋白质的稳定性和聚集性提供一种新的途径，并有助于更好地科学地理解这些问题。通过提供快速且经济高效的方法，在相关温度(储存和生物)下自动进行整个配方研究，研究人员将有实际机会测试更多配方，并选择最适合任何特定生物的配方。

DESCRIPTION (provided by applicant): Protein therapeutics is the fastest growing segment in the biotechnology and pharmaceutical industry with annual sales totaling over $70 billion. Protein therapeutics includes monoclonal antibodies, recombinant proteins, chimeric proteins and other protein receptor constructs. A major hurdle in the development of proteins as pharmaceutical drugs is their formulation in a safe and stable form. The identification of buffer, ligand and excipient conditions that maximize their stability and eliminate protein aggregation is critical during development and often requires the evaluation of hundreds of conditions. This time-consuming task is compounded by the absence of completely automated instruments with the capability of accurately measuring the stability/aggregation matrix of a protein. The goal of this proposal is to develop a fully automated, protein chemical denaturation, fluorescence instrument aimed at measuring multi- dimensional protein stability and aggregation matrices. Unlike any other currently available instrument, this instrument will be capable of automatically preparing and analyzing up to 96 protein denaturation curves - enough to complete an entire formulations study for a new biologic. In this instrument, the user will only need to provide protein and bulk formulation solutions. The instrument will automatically prepare all solutions, perform the measurements, analyze the data and present the results to the investigator. PUBLIC HEALTH RELEVANCE: This instrument will significantly accelerate the development of protein therapeutics and find a significant market. In addition, it will provide a new way to study protein stability and aggregation, and contribute to the development of a better scientific understanding of these issues. By providing a rapid and cost-effective means to automatically conduct an entire Formulations Study at relevant temperatures (storage and biological), researchers will have the practical opportunity to test more Formulations and to select the Formulation that is optimal for any specific biologic.