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The Pharmacokinetics of Fumaric Acid Esters Reveal Their In Vivo Effects
Trends in Pharmacological Sciences ( IF 13.8 ) Pub Date : 2017-11-25 , DOI: 10.1016/j.tips.2017.11.002
Ulrich Mrowietz , Peter John Morrison , Ina Suhrkamp , Margaret Kumanova , Bernd Clement

Fumaric acid ester-based drugs are used for the treatment of psoriasis and multiple sclerosis. All licensed fumaric acid ester drugs contain dimethylfumarate (DMF) as the main active component. Due to the expanding use of oral DMF there is growing scientific interest in determining its as-yet-unknown mechanism of action. However, the pharmacology and chemistry of DMF are often not fully considered in the design and interpretation of experiments; namely, that while DMF is plasma-membrane permeable and has strong effects on many cell types in vitro, it is rapidly metabolized into membrane-impermeable monomethylfumarate (MMF) in vivo. This can lead to significant biological effects being erroneously assigned to DMF. Understanding the pharmacology of DMF means that future work can more closely reflect the state in vivo.



中文翻译:

富马酸酯的药代动力学揭示了它们的体内作用

基于富马酸酯的药物用于治疗牛皮癣和多发性硬化症。所有获得许可的富马酸酯药物均含有富马酸二甲酯(DMF)作为主要活性成分。由于口服DMF的广泛使用,人们对确定其迄今未知的作用机理的兴趣日益浓厚。但是,DMF的药理学和化学常在实验的设计和解释中并未得到充分考虑。即,虽然DMF是质膜可渗透的并且对许多细胞类型强烈影响在体外,它迅速代谢成不可透过膜的monomethylfumarate(MMF)在体内。这可能会导致将重要的生物学效应错误地分配给DMF。了解DMF的药理学意味着未来的工作可以更紧密地反映体内状态。

更新日期:2017-11-25
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