Adar Liat, Avisar Noa, Lammerich Andreas, Kleiman Robert B, Spiegelstein Ofer
R&D, Teva Pharmaceutical Industries Ltd, Netanya, Israel.
Biosimilars Clinical Development, CPP Teva ratiopharm, Merckle GmbH, Ulm, Germany.
Drug Des Devel Ther. 2015 May 15;9:2653-62. doi: 10.2147/DDDT.S81799. eCollection 2015.
Tbo-filgrastim is a recombinant human granulocyte colony-stimulating factor approved by the US Food and Drug Administration to reduce the duration of severe neutropenia in patients with nonmyeloid malignancies receiving myelosuppressive anticancer drugs associated with a clinically significant incidence of febrile neutropenia. We assessed the effect of tbo-filgrastim on cardiac conduction and repolarization in healthy subjects. A three-arm, parallel-group, active- and placebo-controlled, double-blind study randomized healthy adults to a single 5 μg/kg intravenous tbo-filgrastim infusion, a single intravenous placebo infusion, or a single 400 mg moxifloxacin oral dose. The primary end point was placebo-corrected time-matched change from baseline in QT interval corrected using a QT individual correction (QTcI) method. Secondary end points included heart rate, PR interval, QRS duration, change in electrocardiogram patterns, correlation between QTcI change from baseline (milliseconds) and tbo-filgrastim serum concentrations, and safety variables. A total of 145 subjects were enrolled (50 tbo-filgrastim, 50 placebo, 45 moxifloxacin). Peak placebo-corrected change from baseline for QTcI with tbo-filgrastim was 3.5 milliseconds, with a two-sided 95% upper confidence interval of 7.2 milliseconds, demonstrating no signal for any tbo-filgrastim effect on QTc. Concentration-effect modeling showed no evidence of an effect of tbo-filgrastim on cardiac repolarization. Tbo-filgrastim produced no clinically significant changes in other electrocardiogram parameters. Tbo-filgrastim was well tolerated.
替勃龙非格司亭是一种重组人粒细胞集落刺激因子,已获美国食品药品监督管理局批准,用于缩短接受与发热性中性粒细胞减少症临床显著发生率相关的骨髓抑制性抗癌药物治疗的非髓样恶性肿瘤患者严重中性粒细胞减少的持续时间。我们评估了替勃龙非格司亭对健康受试者心脏传导和复极的影响。一项三臂、平行组、活性药物与安慰剂对照、双盲研究将健康成年人随机分为单次静脉输注5μg/kg替勃龙非格司亭组、单次静脉输注安慰剂组或单次口服400mg莫西沙星组。主要终点是采用QT个体校正(QTcI)方法校正后的QT间期相对于基线的安慰剂校正时间匹配变化。次要终点包括心率、PR间期、QRS时限、心电图模式变化、QTcI相对于基线的变化(毫秒)与替勃龙非格司亭血清浓度之间的相关性以及安全性变量。总共招募了145名受试者(50名替勃龙非格司亭组、50名安慰剂组、45名莫西沙星组)。替勃龙非格司亭组QTcI相对于基线的安慰剂校正峰值变化为3.5毫秒,双侧95%置信上限为7.2毫秒,表明未发现替勃龙非格司亭对QT有任何影响的信号。浓度-效应模型显示没有证据表明替勃龙非格司亭对心脏复极有影响。替勃龙非格司亭在其他心电图参数方面未产生具有临床意义的变化。替勃龙非格司亭耐受性良好。