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健康参与者中马利巴韦对心脏复极影响的评估:全面 QT/QTc 研究。

Evaluation of the Effect of Maribavir on Cardiac Repolarization in Healthy Participants: Thorough QT/QTc Study.

机构信息

Shire, a Takeda Company, Lexington, Massachusetts, USA.

出版信息

Clin Transl Sci. 2020 Nov;13(6):1260-1270. doi: 10.1111/cts.12814. Epub 2020 Jul 4.

Abstract

Maribavir is an orally bioavailable benzimidazole riboside in clinical development for treatment of cytomegalovirus infection in patients who undergo transplantation. Maribavir was evaluated in a thorough QT (TQT) study to determine any effects on cardiac repolarization. The effect of maribavir 100 and 1,200 mg oral doses on the baseline-adjusted and placebo-adjusted corrected QT (QTc) interval (delta delta QTc (ddQTc)) and other electrocardiogram (ECG) parameters was assessed in a randomized, phase I, placebo-controlled, four-period crossover study in healthy participants (men and women ages 18-50 years). Additionally, maribavir pharmacokinetics, safety, and tolerability were investigated. Moxifloxacin (400 mg) was used as a positive control to demonstrate the study's ability to detect QT prolongation. Digital 12-lead Holter ECG monitoring was performed over 22 hours following study drug administration. Individual, Fridericia's, and Bazett's QTc intervals were calculated. Of 52 randomized participants (29 ± 8.1 years old; 31 men (60%)), 50 (96%) completed the study. For both 100-mg and 1200-mg doses of maribavir, analysis of ddQTc demonstrated that the upper bound of the two-sided 90% confidence interval was below the 10-ms threshold at all time points. The concentration-effect analysis demonstrated no relationship between ddQTc and plasma concentrations of maribavir (and its metabolite). There were no clinically meaningful changes in heart rate and systolic blood pressure. The most common adverse event was dysgeusia; no serious adverse events were reported. This TQT study demonstrated that maribavir did not have impact on cardiac repolarization.

摘要

马拉韦罗是一种临床开发中的口服生物可利用苯并咪唑核苷,用于治疗接受移植的患者的巨细胞病毒感染。马拉韦罗在一项全面的 QT(TQT)研究中进行了评估,以确定其对心脏复极的任何影响。一项随机、I 期、安慰剂对照、四周期交叉研究在健康受试者(18-50 岁的男性和女性)中评估了马拉韦罗 100 和 1200mg 口服剂量对基线校正和安慰剂校正的校正 QT(QTc)间隔(delta delta QTc(ddQTc))和其他心电图(ECG)参数的影响。此外,还研究了马拉韦罗的药代动力学、安全性和耐受性。莫西沙星(400mg)被用作阳性对照,以证明该研究检测 QT 延长的能力。给药后 22 小时进行数字 12 导联 Holter ECG 监测。计算个体、Fridericia 和 Bazett 的 QTc 间隔。在 52 名随机参与者(29±8.1 岁;31 名男性(60%))中,有 50 名(96%)完成了研究。对于马拉韦罗的 100mg 和 1200mg 剂量,ddQTc 的分析表明,在所有时间点,双侧面 90%置信区间的上限均低于 10ms 阈值。浓度-效应分析表明,ddQTc 与马拉韦罗(及其代谢物)的血浆浓度之间没有关系。心率和收缩压没有出现有临床意义的变化。最常见的不良事件是味觉障碍;无严重不良事件报告。这项 TQT 研究表明,马拉韦罗对心脏复极没有影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b4b/7719377/d168909d31a8/CTS-13-1260-g001.jpg

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