Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, California 94158, USA; email:
Center for Tuberculosis Research, Johns Hopkins University School of Medicine, Baltimore, Maryland 21231, USA.
Annu Rev Pharmacol Toxicol. 2021 Jan 6;61:495-516. doi: 10.1146/annurev-pharmtox-030920-011143. Epub 2020 Aug 17.
Tuberculosis (TB) kills more people than any other infectious disease. Challenges for developing better treatments include the complex pathology due to within-host immune dynamics, interpatient variability in disease severity and drug pharmacokinetics-pharmacodynamics (PK-PD), and the growing emergence of resistance. Model-informed drug development using quantitative and translational pharmacology has become increasingly recognized as a method capable of drug prioritization and regimen optimization to efficiently progress compounds through TB drug development phases. In this review, we examine translational models and tools, including plasma PK scaling, site-of-disease lesion PK, host-immune and bacteria interplay, combination PK-PD models of multidrug regimens, resistance formation, and integration of data across nonclinical and clinical phases.We propose a workflow that integrates these tools with computational platforms to identify drug combinations that have the potential to accelerate sterilization, reduce relapse rates, and limit the emergence of resistance.
结核病 (TB) 是导致人类死亡的头号传染病。在开发更好的治疗方法上面临诸多挑战,包括宿主内免疫动态导致的复杂病理学、疾病严重程度和药物药代动力学-药效学 (PK-PD) 在患者间的差异,以及耐药性的不断出现。使用定量和转化药理学的模型指导药物研发已越来越被视为一种能够对药物进行优先级排序和方案优化的方法,可有效推进化合物通过结核病药物研发各阶段。在本文综述中,我们研究了转化模型和工具,包括血浆 PK 比例缩放、病变部位 PK、宿主免疫和细菌相互作用、多药联合 PK-PD 模型、耐药形成以及非临床和临床阶段数据的整合。我们提出了一个工作流程,将这些工具与计算平台集成,以识别具有潜在潜力的药物组合,从而加速杀菌、降低复发率并限制耐药性的出现。