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单剂量和超治疗剂量的拉罗匹仑,一种选择性前列腺素 D2 受体 1 拮抗剂,不会延长健康志愿者的 QTcF 间期。

Single therapeutic and supratherapeutic doses of laropiprant, a selective prostaglandin D2 receptor 1 antagonist, do not prolong the QTcF interval in healthy volunteers.

机构信息

Merck Research Laboratories, Rahway, New Jersey, USA.

出版信息

J Clin Pharmacol. 2010 Nov;50(11):1273-9. doi: 10.1177/0091270009360042. Epub 2010 Jan 27.

DOI:10.1177/0091270009360042
PMID:20107202
Abstract

Laropiprant (LRPT), a prostaglandin D(2) receptor-1 antagonist shown to reduce niacin-induced flushing symptoms, has been combined with niacin for treatment of dyslipidemia. This study evaluated the effects of LRPT (50 mg and 600 mg, respectively) on the QT interval with Fridericia's correction (QTcF). QTcF measurements were made over a 24-hour period following administration of single-dose moxifloxacin 400 mg, LRPT 50 mg, LRPT 600 mg, or placebo. The primary hypothesis was supported if the 90% confidence intervals (CIs) for the least squares (LS) mean differences between placebo and LRPT in change from baseline in QTcF interval were <10 milliseconds at every time point. The upper limits of the 90% CIs for LS mean differences from placebo in changes from baseline in QTcF intervals for LRPT 50 mg and 600 mg were <5 milliseconds at every time point. The lower limits of the 90% CIs for placebo-adjusted LS mean changes from baseline in QTcF intervals for moxifloxacin exceeded 0 milliseconds at every time point, demonstrating the sensitivity of this assay to detect increases in the QTcF interval. In conclusion, single doses of LRPT 50 mg and 600 mg do not prolong the QTcF interval relative to placebo and are generally well tolerated.

摘要

拉罗匹坦(LRPT)是一种前列腺素 D2 受体-1 拮抗剂,已被证明可减少烟酸引起的潮红症状,与烟酸联合用于治疗血脂异常。本研究评估了 LRPT(分别为 50mg 和 600mg)对 Fridericia 校正 QT 间期(QTcF)的影响。在单次给予莫西沙星 400mg、LRPT 50mg、LRPT 600mg 或安慰剂后 24 小时内进行 QTcF 测量。如果安慰剂和 LRPT 在 QTcF 间隔从基线变化的最小二乘(LS)均值差异的 90%置信区间(CI)在每个时间点均<10 毫秒,则支持主要假设。LRPT 50mg 和 600mg 的 LS 均值差异从基线的 QTcF 间隔变化的 90%CI 的上限在每个时间点均<5 毫秒。莫西沙星的安慰剂调整 LS 均值变化从 QTcF 间隔的基线的 90%CI 的下限在每个时间点均超过 0 毫秒,表明该测定法对 QTcF 间隔的增加具有敏感性。总之,LRPT 50mg 和 600mg 的单剂量不会使 QTcF 间隔相对于安慰剂延长,并且通常耐受良好。

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