InsightRX, 548 Market St. #88083, San Francisco, CA, 94104, USA.
Department of Clinical Pharmacy, University of California, San Francisco, CA, USA.
J Pharmacokinet Pharmacodyn. 2024 Jun;51(3):279-288. doi: 10.1007/s10928-024-09915-w. Epub 2024 Mar 23.
Dose personalization improves patient outcomes for many drugs with a narrow therapeutic index and high inter-individuality variability, including busulfan. Non-compartmental analysis (NCA) and model-based methods like maximum a posteriori Bayesian (MAP) approaches are two methods routinely used for dose optimization. These approaches vary in how they estimate patient-specific pharmacokinetic parameters to inform a dose and the impact of these differences is not well-understood. Using busulfan as an example application and area under the concentration-time curve (AUC) as a target exposure metric, these estimation methods were compared using retrospective patient data (N = 246) and simulated precision dosing treatment courses. NCA was performed with or without peak extension, and MAP Bayesian estimation was performed using either the one-compartment Shukla model or the two-compartment McCune model. All methods showed good agreement on real-world data (correlation coefficients of 0.945-0.998) as assessed by Bland-Altman plots, although agreement between NCA and MAP methods was higher during the first dosing interval (0.982-0.994) compared to subsequent dosing intervals (0.918-0.938). In dose adjustment simulations, both NCA and MAP estimated high target attainment (> 98%) although true simulated target attainment was lower for NCA (63-66%) versus MAP (91-93%). The largest differences in AUC estimation were due to different assumptions for the shape of the concentration curve during the infusion phase, followed by how the methods considered time-dependent clearance and concentration-time points collected in earlier intervals. In conclusion, although AUC estimates between the two methods showed good correlation, in a simulated study, MAP lead to higher target attainment. When changing from one method to another, or changing infusion duration and other factors, optimum estimated exposure targets may require adjusting to maintain a consistent exposure.
药物个体化可改善许多治疗指数较窄且个体间变异性较高的药物(包括白消安)的患者结局。非房室分析(NCA)和基于模型的方法(如最大后验贝叶斯(MAP)方法)是常规用于剂量优化的两种方法。这些方法在估计患者特定药代动力学参数以指导剂量方面存在差异,而这些差异的影响尚不清楚。以白消安为例,使用浓度-时间曲线下面积(AUC)作为目标暴露指标,通过回顾性患者数据(N=246)和模拟的精确剂量治疗过程比较这些估计方法。NCA 可在有无峰延伸的情况下进行,MAP 贝叶斯估计可使用单室 Shukla 模型或双室 McCune 模型进行。通过 Bland-Altman 图评估,所有方法在真实数据上均显示出良好的一致性(相关系数为 0.945-0.998),尽管 NCA 和 MAP 方法在首次给药间隔内的一致性更高(0.982-0.994),而在后序给药间隔内则较低(0.918-0.938)。在剂量调整模拟中,NCA 和 MAP 均估计达到高目标浓度(>98%),尽管 NCA 的真实模拟目标浓度较低(63-66%),而 MAP 则较高(91-93%)。AUC 估计值的最大差异归因于输注阶段浓度曲线形状的不同假设,其次是方法如何考虑时间依赖性清除率和早期间隔采集的浓度-时间点。总之,尽管两种方法的 AUC 估计值之间相关性良好,但在模拟研究中,MAP 导致更高的目标浓度。当从一种方法转换为另一种方法,或改变输注持续时间和其他因素时,为维持一致的暴露量,可能需要调整最佳估计的暴露目标。