AbbVie, Inc., North Chicago, Illinois, USA.
Centre for Health Protection, National Institute for Public Health and the Environment (RIVM), Bilthoven, The Netherlands.
Environ Mol Mutagen. 2021 Nov;62(9):512-525. doi: 10.1002/em.22467. Epub 2021 Nov 22.
We present a hypothetical case study to examine the use of a next-generation framework developed by the Genetic Toxicology Technical Committee of the Health and Environmental Sciences Institute for assessing the potential risk of genetic damage from a pharmaceutical perspective. We used etoposide, a genotoxic carcinogen, as a representative pharmaceutical for the purposes of this case study. Using the framework as guidance, we formulated a hypothetical scenario for the use of etoposide to illustrate the application of the framework to pharmaceuticals. We collected available data on etoposide considered relevant for assessment of genetic toxicity risk. From the data collected, we conducted a quantitative analysis to estimate margins of exposure (MOEs) to characterize the risk of genetic damage that could be used for decision-making regarding the predefined hypothetical use. We found the framework useful for guiding the selection of appropriate tests and selecting relevant endpoints that reflected the potential for genetic damage in patients. The risk characterization, presented as MOEs, allows decision makers to discern how much benefit is critical to balance any adverse effect(s) that may be induced by the pharmaceutical. Interestingly, pharmaceutical development already incorporates several aspects of the framework per regulations and health authority expectations. Moreover, we observed that quality dose response data can be obtained with carefully planned but routinely conducted genetic toxicity testing. This case study demonstrates the utility of the next-generation framework to quantitatively model human risk based on genetic damage, as applicable to pharmaceuticals.
我们提出了一个假设性案例研究,以检查使用下一代框架,该框架由健康和环境科学研究所的遗传毒理学技术委员会开发,用于从药物学角度评估遗传损伤的潜在风险。我们使用依托泊苷作为一个基因毒性致癌药物,作为本案例研究的代表药物。使用该框架作为指导,我们制定了一个依托泊苷使用的假设性方案,以说明该框架在药物学中的应用。我们收集了可用于评估遗传毒性风险的依托泊苷相关数据。从收集的数据中,我们进行了定量分析,以估计暴露量(MOE),以描述遗传损伤的风险,这些风险可用于针对预设的假设性用途做出决策。我们发现该框架有助于指导选择适当的测试和选择反映患者遗传损伤潜力的相关终点。以 MOE 形式呈现的风险特征描述允许决策者辨别出有多少益处对于平衡药物可能引起的任何不利影响(如果有)至关重要。有趣的是,药物开发已经根据法规和健康管理机构的期望纳入了该框架的几个方面。此外,我们观察到可以通过精心计划但常规进行的遗传毒性测试获得高质量的剂量反应数据。本案例研究证明了下一代框架在基于遗传损伤定量建模人类风险方面的实用性,适用于药物学。