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“一步法”分析用于 QT 分析可提高非临床 QTc 分析的灵敏度。

The "One-Step" approach for QT analysis increases the sensitivity of nonclinical QTc analysis.

机构信息

Eli Lilly and Company, Indianapolis, Indiana, USA.

Charles River Laboratories, Mattawan, Michigan, USA.

出版信息

Clin Transl Sci. 2023 Nov;16(11):2253-2264. doi: 10.1111/cts.13625. Epub 2023 Sep 19.

Abstract

Whether a compound prolongs cardiac repolarization independent of changes in beat rate is a critical question in drug research and development. Current practice is to resolve this in two steps. First, the QT interval is corrected for the influence of rate and then statistical significance is tested. There is renewed interest in improving the sensitivity of nonclinical corrected QT interval (QTc) assessment with modern studies having greater data density than previously utilized. The current analyses examine the effects of moxifloxacin or vehicle on the QT interval in nonhuman primates (NHPs) using a previously described one-step method. The primary end point is the statistical sensitivity of the assessment. Publications suggest that for a four animal crossover (4 × 4) in NHPs the minimal detectable difference (MDD) is greater than or equal to 10 ms, whereas in an eight animal crossover the MDD is ~6.5 ms. Using the one-step method, the MDD for the four animal NHP assessments was 3 ms. In addition, the one-step model accounted for day-to-day differences in the heart rate and QT-rate slope as well as drug-induced changes in these parameters. This method provides an increase in the sensitivity and reduces the number of animals necessary for detecting potential QT change and represents "best practice" in nonclinical QTc assessment in safety pharmacology studies.

摘要

化合物是否会在不改变心率的情况下延长心脏复极,这是药物研发中的一个关键问题。目前的做法是分两步解决这个问题。首先,校正 QT 间期受心率影响,然后进行统计学意义检验。随着现代研究的数据密度比以前利用的更大,人们对提高非临床校正 QT 间期(QTc)评估的灵敏度重新产生了兴趣。目前的分析使用以前描述的一步法检查莫西沙星或载体对非人灵长类动物(NHP)QT 间期的影响。主要终点是评估的统计灵敏度。出版物表明,对于 4 只动物交叉(4×4)NHP,最小可检测差异(MDD)大于或等于 10ms,而在 8 只动物交叉中,MDD 约为 6.5ms。使用一步法,4 只 NHP 评估的 MDD 为 3ms。此外,一步模型还考虑了心率和 QT 率斜率的日常差异以及这些参数的药物诱导变化。该方法提高了灵敏度,并减少了检测潜在 QT 变化所需的动物数量,代表了安全药理学研究中非临床 QTc 评估的“最佳实践”。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/711e/10651649/bbdb82cc2ced/CTS-16-2253-g001.jpg

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