受体占有率在药物开发中的意义及其基于流式细胞术的方法建立

Application significance of receptor occupancy study and its establishment based onflow cytometry

对于靶向细胞抗原的、基于蛋白质的大分子生物药物而言,评估药物的受体占有率(RO)已经成为其生物标志物组合研究中的关键部分,但该研究在药物开发中的方法验证标准目前还未达成共识,面临着许多技术和操作方面的挑战。在评估RO的多种检测方法中,流式细胞术(FCM)是其主要研究方法之一。本文主要介绍了RO在药物开发中的应用意义,以及基于流式细胞术对大分子生物药物RO的方法建立提出综合性建议。

For protein-based macromolecular biologic drugs targeting cellular antigens,evaluating receptor occupancy(RO)of drugs has become a key part of biomarker combination research.However,no consensus has been reached on the method validation standard of this research in drug development.There are many technical and operational challenges.Flow cytometry(FCM)is one of the main methods for evaluating RO.This article mainly introduces the application significance of RO in drug development,and puts forward comprehensive suggestions on the method establishment of macromolecular biological drug RO based on flow cytometry.