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评估口服细胞分裂周期7激酶抑制剂TAK-931对晚期实体瘤患者QTc间期的影响。

Assessment of Effects of Investigational TAK-931, an Oral Cell Division Cycle 7 Kinase Inhibitor on the QTc Intervals in Patients With Advanced Solid Tumors.

作者信息

Zhou Xiaofei, Diderichsen Paul Matthias, Gupta Neeraj

机构信息

Quantitative Clinical Pharmacology, Takeda Development Center Americas, Inc., Cambridge, Massachusetts, USA.

Certara USA, Inc., Princeton, New Jersey, USA.

出版信息

Clin Pharmacol Drug Dev. 2022 Jun;11(6):770-779. doi: 10.1002/cpdd.1075. Epub 2022 Feb 20.

Abstract

TAK-931, a novel, selective, small-molecule inhibitor of cell division cycle 7 has been investigated in multiple clinical trials in patients with advanced solid tumors. An integrated analysis using data from 2 clinical studies assessed effects of TAK-931 on electrocardiogram QT intervals and heart rate (HR). Pharmacokinetic samples and matched triplicate electrocardiogram data were collected in 48 patients with cancer receiving oral administration of TAK-931 50 or 80 mg once daily. The relationships between TAK-931 plasma concentrations and the HR-corrected QT interval via Fridericia (QTcF) or population (QTcP) and HR were analyzed using linear mixed-effects models with fixed effects for day and time. At the geometric mean maximum TAK-931 plasma concentrations after administration of 50 mg, an HR change of 3.40 beats per minute (90%CI, 1.86-4.80) was predicted. Change in QTcF of -3.41 milliseconds (90%CI, -5.77 to -1.17) and QTcP of -2.02 milliseconds (90%CI, -4.15 to 0.0679) were estimated, indicating there was no effect of TAK-931 on the QT intervals at a recommended phase 2 dose of 50 mg once daily for 14 days in a 21-day cycle.

摘要

TAK-931是一种新型、选择性、小分子细胞分裂周期7抑制剂,已在晚期实体瘤患者中进行了多项临床试验。一项使用两项临床研究数据的综合分析评估了TAK-931对心电图QT间期和心率(HR)的影响。在48例接受TAK-931 50或80mg每日一次口服给药的癌症患者中收集了药代动力学样本和匹配的三份心电图数据。使用具有日和时间固定效应的线性混合效应模型分析TAK-931血浆浓度与通过弗里德里西亚法(QTcF)或群体法(QTcP)校正的QT间期以及心率之间的关系。在给予50mg后TAK-931血浆浓度的几何平均最大值时,预测心率变化为每分钟3.40次搏动(90%CI,1.86-4.80)。估计QTcF变化为-3.41毫秒(90%CI,-5.77至-1.17),QTcP变化为-2.02毫秒(90%CI,-4.15至0.0679),这表明在21天周期中,推荐的2期剂量为每日一次50mg,共14天,TAK-931对QT间期无影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7183/9306994/4b400a4445b4/CPDD-11-770-g002.jpg

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