Ait-Oudhia Sihem, Ovacik Meric Ayse, Mager Donald E
a Center for Pharmacometrics and Systems Pharmacology, Department of Pharmaceutics , College of Pharmacy, University of Florida , Orlando , FL , USA.
b Department of Pharmaceutical Sciences , University at Buffalo, State University of New York , Buffalo , NY , USA.
MAbs. 2017 Jan;9(1):15-28. doi: 10.1080/19420862.2016.1238995. Epub 2016 Sep 23.
Pharmacokinetic (PK) and pharmacodynamic (PD) models seek to describe the temporal pattern of drug exposures and their associated pharmacological effects produced at micro- and macro-scales of organization. Antibody-based drugs have been developed for a large variety of diseases, with effects exhibited through a comprehensive range of mechanisms of action. Mechanism-based PK/PD and systems pharmacology models can play a major role in elucidating and integrating complex antibody pharmacological properties, such as nonlinear disposition and dynamical intracellular signaling pathways triggered by ligation to their cognate targets. Such complexities can be addressed through the use of robust computational modeling techniques that have proven powerful tools for pragmatic characterization of experimental data and for theoretical exploration of antibody efficacy and adverse effects. The primary objectives of such multi-scale mathematical models are to generate and test competing hypotheses and to predict clinical outcomes. In this review, relevant systems pharmacology and enhanced PD (ePD) models that are used as predictive tools for antibody-based drug action are reported. Their common conceptual features are highlighted, along with approaches used for modeling preclinical and clinically available data. Key examples illustrate how systems pharmacology and ePD models codify the interplay among complex biology, drug concentrations, and pharmacological effects. New hybrid modeling concepts that bridge cutting-edge systems pharmacology models with established PK/ePD models will be needed to anticipate antibody effects on disease in subpopulations and individual patients.
药代动力学(PK)和药效动力学(PD)模型旨在描述药物暴露的时间模式及其在微观和宏观组织尺度上产生的相关药理作用。基于抗体的药物已针对多种疾病开发,其作用通过广泛的作用机制表现出来。基于机制的PK/PD和系统药理学模型在阐明和整合复杂的抗体药理学特性方面可发挥重要作用,例如非线性处置和与其同源靶点结合触发的动态细胞内信号通路。可以通过使用强大的计算建模技术来解决此类复杂性,这些技术已被证明是用于实验数据务实表征以及抗体疗效和不良反应理论探索的有力工具。此类多尺度数学模型的主要目标是生成和检验相互竞争的假设并预测临床结果。在本综述中,报告了用作基于抗体药物作用预测工具的相关系统药理学和增强型PD(ePD)模型。突出了它们的共同概念特征,以及用于对临床前和临床可用数据进行建模的方法。关键示例说明了系统药理学和ePD模型如何编纂复杂生物学、药物浓度和药理作用之间的相互作用。需要新的混合建模概念,将前沿的系统药理学模型与已建立的PK/ePD模型联系起来,以预测抗体对亚群和个体患者疾病的影响。