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在转基因小鼠中,PXR的激活导致与Paxlovid的药物相互作用

Saifei Lei¹, Alice Guo², Jie Lu¹

¹Center for Pharmacogenetics, Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, PA 15261, USA.

Acta pharmaceutica Sinica. B

|November 16, 2023

概括

孕妇X受体 (PXR) 的激活加快了nirmatrelvir的新陈代谢,可能降低了Paxlovid的有效性. 在使用PXR激活药物或草药与Paxlovid在COVID-19患者时建议谨慎使用.

科学领域:

药理学药理学是指药理学的学科.
药物新陈代谢药物新陈代谢
药物相互作用药物相互作用

背景情况:

帕克斯洛维德是尼尔马特里尔维尔 (NMV) 和里托纳维尔 (RTV) 的组合,用于治疗COVID-19.
NMV是活性抗病毒成分,而RTV增强了其药理动力学特征.
了解药物和草药相互作用对于安全使用Paxlovid至关重要.

研究的目的:

为了研究涉及Paxlovid的药物/草药相互作用.
为临床Paxlovid应用提供基于机制的指导.
为了阐明Pregnane X受体 (PXR) 在Paxlovid代谢中的作用.

主要方法:

利用重组的人类细胞染色体P450酶 (CYPs) 来识别NMV代谢途径.
使用Cyp3a-null小鼠证实CYP3A在NMV和RTV代谢中的作用.
使用表达人类PXR和CYP3A4/5.5的转基因小鼠模型研究PXR激活效应.

主要成果:

确认CYP3A4和CYP3A5是NMV代谢的主要酶.
证明CYP3A缺陷显著降低了NMV和RTV代谢.
显示PXR激活可调节CYP3A4/5,加速NMV代谢并降低全身暴露.

结论:

激活PXR显著影响了Paxlovid的代谢.
激活PXR的药物和草药可以导致与Paxlovid的药物相互作用.
建议在COVID-19患者中谨慎地同时使用PXR激活物质和Paxlovid.

关键词:

在CYP3A4/5中使用.药物/草药相互作用药物相互作用尼尔马特里尔维尔 (Nirmatrelvir) 是一种帕克斯洛维的使用方法孕妇的X受体受体.莱恩科菲林线 (Rhynchophylline) 是一个临界线.里法皮辛 (Rifampicin) 是一种药物.里托纳维尔 (Ritonavir) 是一种药物.

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