Department of Pharmaceutical Biosciences, Uppsala University, Sweden.
School of Pharmaceutical Sciences, Universiti Sains Malaysia, Malaysia.
CPT Pharmacometrics Syst Pharmacol. 2017 Oct;6(10):686-694. doi: 10.1002/psp4.12214. Epub 2017 Sep 25.
In antihyperglycemic drug development, drug effects are usually characterized using glucose provocations. Analyzing provocation data using pharmacometrics has shown powerful, enabling small studies. In preclinical drug development, high power is attractive due to the experiment sizes; however, insulin is not always available, which potentially impacts power and predictive performance. This simulation study was performed to investigate the implications of performing model-based drug characterization without insulin. The integrated glucose-insulin model was used to simulate and re-estimated oral glucose tolerance tests using a crossover design of placebo and study compound. Drug effects were implemented on seven different mechanisms of action (MOA); one by one or in two-drug combinations. This study showed that exclusion of insulin may severely reduce the power to distinguish the correct from competing drug effect, and to detect a primary or secondary drug effect, however, it did not affect the predictive performance of the model.
在抗高血糖药物开发中,通常使用葡萄糖激发来描述药物作用。使用药物代谢动力学分析激发数据显示出强大的功能,使小研究成为可能。在临床前药物开发中,由于实验规模较大,高功效很有吸引力;然而,胰岛素并不总是可用的,这可能会影响功效和预测性能。本模拟研究旨在探讨在没有胰岛素的情况下进行基于模型的药物特征描述的影响。使用整合的葡萄糖-胰岛素模型模拟并重新估计了使用安慰剂和研究化合物的交叉设计的口服葡萄糖耐量试验。药物作用在七种不同的作用机制(MOA)上实施;一种一种或两种药物组合。这项研究表明,排除胰岛素可能会严重降低区分正确和竞争药物作用的功效,并检测主要或次要药物作用,然而,它并不影响模型的预测性能。