Raptor Pharm & Tox, Ltd, Apex, NC, USA.
ADAMA Deutschland GmbH, Germany.
Regul Toxicol Pharmacol. 2024 Aug;151:105663. doi: 10.1016/j.yrtph.2024.105663. Epub 2024 Jun 12.
As the United States and the European Union continue their steady march towards the acceptance of new approach methodologies (NAMs), we need to ensure that the available tools are fit for purpose. Critics will be well-positioned to caution against NAMs acceptance and adoption if the tools turn out to be inadequate. In this paper, we focus on Quantitative Structure Activity-Relationship (QSAR) models and highlight how the training database affects quality and performance of these models. Our analysis goes to the point of asking, "are the endpoints extracted from the experimental studies in the database trustworthy, or are they false negatives/positives themselves?" We also discuss the impacts of chemistry on QSAR models, including issues with 2-D structure analyses when dealing with isomers, metabolism, and toxicokinetics. We close our analysis with a discussion of challenges associated with translational toxicology, specifically the lack of adverse outcome pathways/adverse outcome pathway networks (AOPs/AOPNs) for many higher tier endpoints. We recognize that it takes a collaborate effort to build better and higher quality QSAR models especially for higher tier toxicological endpoints. Hence, it is critical to bring toxicologists, statisticians, and machine learning specialists together to discuss and solve these challenges to get relevant predictions.
随着美国和欧盟继续稳步接受新方法方法 (NAMs),我们需要确保可用的工具符合目的。如果这些工具被证明是不充分的,批评者将有充分的理由对 NAMs 的接受和采用提出警告。在本文中,我们专注于定量构效关系 (QSAR) 模型,并强调了培训数据库如何影响这些模型的质量和性能。我们的分析甚至问到,“数据库中从实验研究中提取的终点是否可信,或者它们本身是否是假阴性/阳性?”我们还讨论了化学对 QSAR 模型的影响,包括在处理异构体、代谢和毒代动力学时 2-D 结构分析的问题。我们的分析以讨论与转化毒理学相关的挑战结束,特别是对于许多更高层次的终点,缺乏不良结局途径/不良结局途径网络 (AOPs/AOPNs)。我们认识到,建立更好和更高质量的 QSAR 模型,特别是针对更高层次的毒理学终点,需要协作努力。因此,至关重要的是让毒理学家、统计学家和机器学习专家聚集在一起,讨论和解决这些挑战,以获得相关的预测。