跨越障碍：建模药物穿透血脑屏障。
Jumping the Barrier: Modeling Drug Penetration across the Blood-Brain Barrier.
机构信息
Clinical Pharmacology Program, National Cancer Institute, National Institutes of Health, Bethesda, Maryland.
Genitourinary Malignancies Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, Maryland.
出版信息
Clin Cancer Res. 2017 Dec 15;23(24):7437-7439. doi: 10.1158/1078-0432.CCR-17-2741. Epub 2017 Oct 10.
Abstract
Determining the penetration of drugs across the blood-brain barrier is a significant challenge in central nervous system drug development. The use of a mechanistic physiologically based pharmacokinetic model can predict drug exposures in the brain without needing drug measurements. .
摘要
确定药物穿过血脑屏障的渗透是中枢神经系统药物开发中的一个重大挑战。使用基于机制的生理药代动力学模型可以预测大脑中的药物暴露，而不需要药物测量。
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本文引用的文献
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2
Development of a permeability-limited model of the human brain and cerebrospinal fluid (CSF) to integrate known physiological and biological knowledge: Estimating time varying CSF drug concentrations and their variability using in vitro data.建立一个人类大脑和脑脊液（CSF）的通透性受限模型以整合已知的生理和生物学知识：利用体外数据估计随时间变化的脑脊液药物浓度及其变异性。
Drug Metab Pharmacokinet. 2016 Jun;31(3):224-33. doi: 10.1016/j.dmpk.2016.03.005. Epub 2016 Apr 4.
3
The Efficacy of the Wee1 Inhibitor MK-1775 Combined with Temozolomide Is Limited by Heterogeneous Distribution across the Blood-Brain Barrier in Glioblastoma.Wee1抑制剂MK-1775与替莫唑胺联合使用的疗效受胶质母细胞瘤中血脑屏障异质性分布的限制。
Clin Cancer Res. 2015 Apr 15;21(8):1916-24. doi: 10.1158/1078-0432.CCR-14-2588. Epub 2015 Jan 21.
4
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5
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