Li Meizhen, Qiang Wei, Wen Zhou, Li Linling, Wang Lei, Cheng Zeneng
Research Institute of Drug Metabolism and Pharmacokinetics, School of Pharmaceutical Sciences, Central South University, Changsha, Hunan 410013, China.
M. L. and W. Q. contributed equally to this work.
Iran J Pharm Res. 2019 Summer;18(3):1147-1155. doi: 10.22037/ijpr.2019.1100716.
Complex pharmacokinetic (PK) properties including nonlinear elimination were encountered by some monoclonal antibodies (mAbs), and classic compartment models sometimes failed to appropriately describe those properties. In this work, a new model was built on a comprehensive analysis of the complex elimination of mAbs. This new model was firstly utilized to fit with the single-dose plasma concentration data of bevacizumab in beagle dogs receiving an intravenous administration of 2.5 mg/kg bevacizumab. Then, the optimal PK parameters from fitting with the single-dose PK data were employed into the multiple-dose mathematical expressions to predict bevacizumab's multiple-dose PK profiles. One-compartment model recommended as the optimal classic model by DAS 2.0 software was set as a control. As a result, new model fitted better with the single-dose PK profiles of bevacizumab with smaller weighted residual sum of squares and higher fitting degree compared with the classic model. Importantly, new model also accurately predicted the multiple-dose PK profiles of bevacizumab and performed well at the single-to-multiple transition. In conclusion, the new model reasonably explained the complex elimination of bevacizumab, and it might play a big role in the PK studies of bevacizumab and other mAbs.
一些单克隆抗体(mAb)具有包括非线性消除在内的复杂药代动力学(PK)特性,经典房室模型有时无法恰当地描述这些特性。在本研究中,在对mAb复杂消除进行全面分析的基础上建立了一个新模型。该新模型首先用于拟合接受2.5mg/kg贝伐单抗静脉给药的比格犬中贝伐单抗的单剂量血浆浓度数据。然后,将单剂量PK数据拟合得到的最佳PK参数代入多剂量数学表达式中,以预测贝伐单抗的多剂量PK曲线。将DAS 2.0软件推荐的一室模型作为最佳经典模型作为对照。结果,与经典模型相比,新模型对贝伐单抗单剂量PK曲线的拟合效果更好,加权残差平方和更小,拟合度更高。重要的是,新模型还准确预测了贝伐单抗的多剂量PK曲线,并且在单剂量到多剂量转换时表现良好。总之,新模型合理地解释了贝伐单抗的复杂消除过程,可能在贝伐单抗及其他mAb的PK研究中发挥重要作用。