Freie Universität Berlin, Institute of Pharmacy (Pharmacology and Toxicology), Berlin, Germany.
Handb Exp Pharmacol. 2021;265:29-56. doi: 10.1007/164_2020_374.
Preclinical research struggles with its predictive power for drug effects in patients. The clinical success of preclinically approved drug candidates ranges between 3% and 33%. Regardless of the approach, novel disease models and test methods need to prove their relevance and reliability for predicting drug effects in patients, which is usually achieved by method validation. Nevertheless, validating all models appears unrealistic due to the variety of diseases. Thus, novel concepts are needed to increase the quality of preclinical research.Herein, we introduce qualification as a minimal standard to establish the relevance of preclinical models and test methods. Qualification starts with prioritizing and translating scientific requirements into technical parameters by quality function deployment. Qualified models use authenticated cells, which resemble the corresponding cells in humans in morphology and drug target expression. Moreover, disease models differ from normal models in the expression of relevant biomarkers. As a result, qualified test methods can discriminate effects of treatment standards and the effects of weakly effective or ineffective substances. Observer-blind readout, adequate data documentation, dropout inclusion, and a priori power studies are as crucial as realistic dosage regimens for qualified approaches. Here, we showcase the implementation of qualification. Adjusting the level of model complexity and qualification to three defined phases of preclinical research assures the optimal level of certainty at each step.In conclusion, qualification strengthens the researchers' impact by defining basic requirements that novel approaches must fulfill while still allowing for scientific creativity. Qualification helps to improve the predictive power of preclinical research. Applied to human cell-based models, qualification reduces animal testing, since only effective drug candidates are subjected to final animal testing and subsequently to clinical trials.
临床前研究在预测药物对患者的疗效方面存在困难。临床前批准的候选药物的临床成功率在 3%至 33%之间。无论采用哪种方法,新型疾病模型和测试方法都需要证明其对预测患者药物疗效的相关性和可靠性,这通常通过方法验证来实现。然而,由于疾病种类繁多,验证所有模型似乎不切实际。因此,需要新的概念来提高临床前研究的质量。
在这里,我们引入资格作为建立临床前模型和测试方法相关性的最低标准。资格从优先考虑和通过质量功能部署将科学要求转化为技术参数开始。合格的模型使用经过认证的细胞,这些细胞在形态和药物靶标表达方面与人类相应的细胞相似。此外,疾病模型在相关生物标志物的表达上与正常模型不同。因此,合格的测试方法可以区分治疗标准的效果和弱效或无效物质的效果。观察者盲读、充分的数据记录、纳入辍学者以及事先进行的效能研究与合格方法的现实剂量方案同样重要。在这里,我们展示了资格的实施。根据临床前研究的三个定义阶段调整模型复杂性和资格水平,可确保在每个步骤都达到最佳的确定性水平。
总之,资格通过定义新方法必须满足的基本要求来增强研究人员的影响力,同时仍允许发挥科学创造力。资格有助于提高临床前研究的预测能力。应用于基于人类细胞的模型,资格减少了动物试验,因为只有有效的药物候选物才会进行最终的动物试验,然后进行临床试验。