Li Claire H, Sherer Eric A, Lewis Lionel D, Bies Robert R
Indiana University School of Medicine, Indianapolis, IN, USA; Indiana Clinical and Translational Sciences Institute (CTSI), Indianapolis, IN, USA.
J Clin Pharmacol. 2015 May;55(5):556-62. doi: 10.1002/jcph.449. Epub 2015 Feb 4.
The objectives of this study were to determine (1) the accuracy with which individual patient level exposure can be determined and (2) whether a known food effect can be identified in a trial simulation of a typical population pharmacokinetic trial. Clinical trial simulations were undertaken using NONMEM VII to assess a typical oncology pharmacokinetic trial design. Nine virtual trials for each compound were performed for combinations of different levels of between-occasion variability, number of patients in the trial, and magnitude of a food covariate on oral clearance. Less than 5% and 20% bias and precision were obtained in individual clearance estimated for both abiraterone and nilotinib using this design. This design resulted in biased and imprecise population clearance estimates for abiraterone. The between-occasion variability in most trials was captured with less than 30% of percent bias and precision. The food effect was detectable as a statistically significant covariate on oral clearance for abiraterone and nilotinib with percent bias and precision of the food covariate less than 20%. These results demonstrate that clinical trial simulation can be used to explore the ability of specific trial designs to evaluate the power to identify individual and population level exposures, covariate, and variability effects.
(1)确定个体患者水平暴露的准确性;(2)在典型群体药代动力学试验的模拟试验中是否能够识别已知的食物效应。使用NONMEM VII进行临床试验模拟,以评估典型的肿瘤药代动力学试验设计。针对不同水平的给药间隔变异性、试验中的患者数量以及食物协变量对口服清除率的影响大小的组合,对每种化合物进行了9次虚拟试验。使用该设计对阿比特龙和尼洛替尼进行个体清除率估计时,偏差和精密度分别低于5%和20%。该设计导致阿比特龙群体清除率估计出现偏差且不精确。大多数试验中的给药间隔变异性,偏差百分比和精密度均低于30%。对于阿比特龙和尼洛替尼,食物效应作为口服清除率的统计学显著协变量是可检测到的,食物协变量的偏差百分比和精密度均低于20%。这些结果表明,临床试验模拟可用于探索特定试验设计评估识别个体和群体水平暴露、协变量及变异性效应的能力。