Institute of Mathematics, Universität Potsdam, Potsdam, Germany.
Institute of Mathematics, Humboldt-Universität zu Berlin, Berlin, Germany.
CPT Pharmacometrics Syst Pharmacol. 2021 Jun;10(6):564-576. doi: 10.1002/psp4.12614. Epub 2021 Jun 4.
The characterization of covariate effects on model parameters is a crucial step during pharmacokinetic/pharmacodynamic analyses. Although covariate selection criteria have been studied extensively, the choice of the functional relationship between covariates and parameters, however, has received much less attention. Often, a simple particular class of covariate-to-parameter relationships (linear, exponential, etc.) is chosen ad hoc or based on domain knowledge, and a statistical evaluation is limited to the comparison of a small number of such classes. Goodness-of-fit testing against a nonparametric alternative provides a more rigorous approach to covariate model evaluation, but no such test has been proposed so far. In this manuscript, we derive and evaluate nonparametric goodness-of-fit tests for parametric covariate models, the null hypothesis, against a kernelized Tikhonov regularized alternative, transferring concepts from statistical learning to the pharmacological setting. The approach is evaluated in a simulation study on the estimation of the age-dependent maturation effect on the clearance of a monoclonal antibody. Scenarios of varying data sparsity and residual error are considered. The goodness-of-fit test correctly identified misspecified parametric models with high power for relevant scenarios. The case study provides proof-of-concept of the feasibility of the proposed approach, which is envisioned to be beneficial for applications that lack well-founded covariate models.
对模型参数的协变量效应进行特征描述是药代动力学/药效学分析过程中的关键步骤。虽然已经对协变量选择标准进行了广泛的研究,但协变量与参数之间的函数关系的选择却没有得到太多关注。通常,会根据领域知识或特定的类别(线性、指数等)来选择协变量与参数之间的关系,并且统计评估仅限于对少数此类关系类别的比较。与非参数替代方案相比,通过拟合优度检验可以提供更严格的协变量模型评估方法,但到目前为止还没有提出这样的检验方法。在本文中,我们推导并评估了针对参数协变量模型的非参数拟合优度检验,针对零假设,提出了一种基于核正则化的替代方案,将统计学习中的概念应用于药理学领域。该方法在针对单克隆抗体清除率的年龄依赖性成熟效应的估计的模拟研究中进行了评估,考虑了数据稀疏性和残差误差变化的情况。拟合优度检验对具有高相关场景的参数模型的错误指定具有很高的功效。该案例研究证明了所提出方法的可行性,该方法有望为缺乏良好协变量模型的应用提供帮助。