National Heart and Lung Institute, Imperial College, Dovehouse Street, London, SW3 6LY, England, UK.
Division of Cardiovascular and Renal Products, Office of New Drugs, Center for Drug Evaluation and Research, US Food and Drug Administration, Silver Spring, MD, USA.
J Pharmacokinet Pharmacodyn. 2018 Jun;45(3):491-503. doi: 10.1007/s10928-018-9587-8. Epub 2018 Apr 12.
QT/RR hysteresis and QT/RR adaptation are interlinked but separate physiological processes signifying how quickly and how much QT interval changes when heart rate changes, respectively. While QT interval duration is, as a rule, corrected for heart rate in terms of the QT/RR adaptation, the correction for QT/RR hysteresis is frequently omitted in studies of drug-induced QTc changes. This study used data from previously conducted thorough QT studies to investigate the extent of QTc errors caused by omitting the correction for QT/RR hysteresis, particularly in small clinical investigations. Statistical modeling approach was used to generate 11,000 simulated samples of 10-subject studies in which mixed effect PK/PD models were used to estimate drug-induced QTc changes at mean maximum plasma concentration of investigated compounds. Calculations of QTc intervals involving and omitting QT/RR hysteresis correction were compared. These comparisons showed that ignoring QT/RR hysteresis has two undesirable effects: (A) In the design of subject-specific heart rate corrections (needed in studies of drugs that change heart rate) omission of QT/RR hysteresis may lead to signals of QTc prolongation of more than 10 ms to be missed. (B) Irrespective of whether the investigated drug changes heart rate, omission of QT/RR hysteresis causes the widths of the confidence intervals of the PK/PD predicted QTc interval changes to be increased by 20-30% on average (exceeding 50% in some cases). This may lead to a failure of excluding meaningful QTc prolongation which would be excluded if using hysteresis correction. The study concludes that correction for QT/RR hysteresis should be incorporated into future studies of drug-induced QTc changes. Subject-specific heart rate corrections that omit hysteresis correction may lead to erroneously biased conclusions. Even when using universal (e.g. Fridericia) heart rate correction, hysteresis correction decreases the confidence intervals of QTc changes and thus helps avoiding false positive outcomes.
QT/RR 滞后和 QT/RR 适应是相互关联但又不同的生理过程,分别表示心率变化时 QT 间期变化的快慢和幅度。虽然 QT 间期的持续时间通常根据 QT/RR 适应进行心率校正,但在药物致 QTc 变化的研究中,QT/RR 滞后的校正常常被忽略。本研究使用先前进行的全面 QT 研究的数据,研究了忽略 QT/RR 滞后校正导致的 QTc 误差的程度,特别是在小型临床研究中。采用统计建模方法生成了 10 名受试者研究的 11000 个模拟样本,其中混合效应 PK/PD 模型用于估计研究化合物最大血浆浓度时药物引起的 QTc 变化。比较了涉及和不涉及 QT/RR 滞后校正的 QTc 间隔计算。这些比较表明,忽略 QT/RR 滞后有两个不良影响:(A)在药物改变心率的受试者特异性心率校正的设计中(在研究改变心率的药物时需要),忽略 QT/RR 滞后可能导致错过超过 10ms 的 QTc 延长信号。(B)无论研究药物是否改变心率,忽略 QT/RR 滞后都会导致 PK/PD 预测 QTc 间隔变化的置信区间宽度平均增加 20-30%(在某些情况下超过 50%)。这可能导致无法排除如果使用滞后校正则会排除的有意义的 QTc 延长。该研究得出结论,应将 QT/RR 滞后校正纳入未来的药物致 QTc 变化研究中。忽略滞后校正的受试者特异性心率校正可能导致错误的有偏差的结论。即使使用通用(例如 Fridericia)心率校正,滞后校正也会减小 QTc 变化的置信区间,从而有助于避免假阳性结果。