Electrocardiographic Effects of a Supratherapeutic Dose of WCK 2349, a Benzoquinolizine Fluoroquinolone
摘要
The purpose of this study was to measure the electrocardiographic (ECG) effects of WCK 2349 (the L-alanine ester prodrug of levonadifloxacin) at a supratherapeutic oral dose of 2,600 mg. A total of 48 healthy volunteers were randomized to treatment with placebo, WCK 2349, or oral moxifloxacin, 400 mg, in a crossover-designed thorough QT study. A supratherapeutic mean maximum levonadifloxacin concentration (C-max) of 43.3 mu g/mL was achieved at 3.1 hours. A therapeutic dose of 1,000 mg b.i.d. in a previous study in patients resulted in a C-max of 17.8 mu g/mL. WCK 2349 exerted no significant effect on baseline- and placebo-corrected QTcF (QT interval corrected for heart rate (HR) by the Fridericia formula), QRS, or PR interval. HR was transiently accelerated by a maximum of 14.4 (95% confidence interval, 11.80-16.92) beats per minute (bpm) at 3 hours. Concentration-effect modeling predicted a mean increase of 8.0 bpm at C-max at the standard therapeutic dose. A therapeutic dose of 1,000 mg b.i.d. of WCK 2349 is not expected to cause clinically significant ECG effects, except for a possible transient increase in HR, which seems to be clinically insignificant.展開▼
機譯:本研究的目的是測量WCK 2349(L-丙氨酸酯前藥物的ECG)效應(Levonadifloxacin的L-丙氨酸酯前藥),以2,600mg的Supratterical口服劑量。共有48名健康的志愿者隨機用安慰劑,WCK 2349或口服Moxifloxacin,400毫克進行治療,在交叉設計的徹底QT研究中。在3.1小時的3.1小時達到43.3μg/ ml的SupratTerapeutic的最大左旋酮胺濃度(C-max)。 1,000mg B.I.D的治療劑量。在先前的患者的研究中導致C-MAX為17.8μg/ ml。 WCH 2349對基線和安慰劑校正的QTCF(QT間隔通過Fridericia公式進行了QT間隔(HR),QRS或PR間隔沒有顯著影響。 HR在3小時內(nèi)瞬時加速最多14.4(95%置信區(qū)間,11.80-16.92),每分鐘(BPM)在3小時。濃縮效應建模預測標準治療劑量的C-MAX平均增加8.0bpm。 1,000mg B.I.D的治療劑量。在WCK 2349中預計不會導致臨床顯著的心電圖效應,除了人力資源可能的瞬態(tài)增加,似乎是臨床上微不足道的。展開▼
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