Department of Translational Medicine, Novartis Institutes for BioMedical Research, Basel, Switzerland.
Department of Preclinical Safety, Novartis Institutes for BioMedical Research, Basel, Switzerland.
Clin Transl Sci. 2020 Nov;13(6):1316-1326. doi: 10.1111/cts.12832. Epub 2020 Jul 23.
Umibecestat, an orally active β-secretase inhibitor, reduces the production of amyloid beta-peptide that accumulates in the brain of patients with Alzheimer's disease. The echocardiogram effects of umibecestat, on QTcF (Fridericia-corrected QT), on PR and QRS and heart rate (HR), were estimated by concentration-effect modeling. Three phase I/II studies with durations up to 3 months, with 372 healthy subjects over a wide age range, including both sexes and 2 ethnicities, were pooled, providing a large data set with good statistical power. No clinically relevant effect on QTcF, PR interval, QRS duration, or HR were observed up to supratherapeutic doses. The upper bound of 90% confidence intervals of the ∆QTcF was below the 10 ms threshold of regulatory concern for all concentrations measured. Prespecified sensitivity analysis confirmed the results in both sexes, in those over and below 60 years, and in Japanese subjects. All conclusions were endorsed by the US Food and Drug Administration (FDA).
乌米贝司他是一种口服活性的β-分泌酶抑制剂,可减少阿尔茨海默病患者大脑中堆积的淀粉样β肽的产生。通过浓度效应模型来估计乌米贝司他对 QTcF(Fridericia 校正 QT)、PR 和 QRS 及心率(HR)的心脏超声心动图影响。三项为期 3 个月的 I/II 期研究共纳入了 372 名健康受试者,年龄范围广泛,包括男女和 2 个种族,提供了一个具有良好统计功效的大型数据集。在达到治疗窗上限的剂量下,乌米贝司他对 QTcF、PR 间期、QRS 持续时间或 HR 没有观察到临床相关的影响。在所有测量浓度下,QTcF 的 90%置信区间上限均低于监管关注的 10 毫秒阈值。预先规定的敏感性分析在男女、60 岁以上和以下的人群以及日本受试者中均证实了这些结果。所有结论均得到美国食品和药物管理局(FDA)的认可。