Biovista, 34 Rodopoleos Street, 16777, Athens, Greece.
UCIBIO, REQUIMTE, Laboratory of Toxicology, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, 4050-313, Porto, Portugal.
Arch Toxicol. 2020 Aug;94(8):2829-2845. doi: 10.1007/s00204-020-02788-1. Epub 2020 Jun 5.
Drug-induced Mood- and Cognition-related adverse events (MCAEs) are often only detected during the clinical trial phases of drug development, or even after marketing, thus posing a major safety concern and a challenge for both pharmaceutical companies and clinicians. To fill some gaps in the understanding and elucidate potential biological mechanisms of action frequently associated with MCAEs, we present a unique workflow linking observational population data with the available knowledge at molecular, cellular, and psychopharmacology levels. It is based on statistical analysis of pharmacovigilance reports and subsequent signaling pathway analyses, followed by evidence-based expert manual curation of the outcomes. Our analysis: (a) ranked pharmaceuticals with high occurrence of such adverse events (AEs), based on disproportionality analysis of the FDA Adverse Event Reporting System (FAERS) database, and (b) identified 120 associated genes and common pathway nodes possibly underlying MCAEs. Nearly two-thirds of the identified genes were related to immune modulation, which supports the critical involvement of immune cells and their responses in the regulation of the central nervous system function. This finding also means that pharmaceuticals with a negligible central nervous system exposure may induce MCAEs through dysregulation of the peripheral immune system. Knowledge gained through this workflow unravels putative hallmark biological targets and mediators of drug-induced mood and cognitive disorders that need to be further assessed and validated in experimental models. Thereafter, they can be used to substantially improve in silico/in vitro/in vivo tools for predicting these adversities at a preclinical stage.
药物引起的情绪和认知相关不良事件(MCAEs)通常仅在药物开发的临床试验阶段或甚至在上市后才被发现,因此对制药公司和临床医生都构成了重大安全问题和挑战。为了填补对这些不良事件的理解上的一些空白,并阐明与 MCAEs 经常相关的潜在生物学作用机制,我们提出了一个独特的工作流程,将观察性人群数据与分子、细胞和精神药理学水平上的现有知识联系起来。它基于对药物警戒报告的统计分析和随后的信号通路分析,以及基于证据的专家手动对结果的策展。我们的分析:(a)根据 FDA 不良事件报告系统(FAERS)数据库的不均衡分析,对高发生此类不良事件(AE)的药物进行排名,(b)确定了 120 个相关基因和常见通路节点,这些基因可能是 MCAEs 的潜在基础。所鉴定的基因中有近三分之二与免疫调节有关,这支持免疫细胞及其反应在中枢神经系统功能调节中的关键作用。这一发现还意味着,即使药物对中枢神经系统的暴露程度较低,也可能通过外周免疫系统的失调引起 MCAEs。通过该工作流程获得的知识揭示了药物引起的情绪和认知障碍的潜在标志性生物靶标和介质,这些靶标和介质需要在实验模型中进一步评估和验证。此后,它们可用于大大改进预测这些不良事件的临床前阶段的计算/体外/体内工具。