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首页> 外文期刊>Clinics in dermatology >Fumaric acid esters.
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Fumaric acid esters.

机译：富马酸酯。

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Several clinical studies have shown that systemic therapy with fumaric acid esters (FAEs) in patients with moderate to severe psoriasis is effective and has a good long-term safety profile. For therapeutic use, tablets with a defined mixture of FAEs (dimethylfumarate [DMF] and three different salts of monoethylfumarate) are registered in Germany. There is evidence that DMF is the most essential component in this formulation with an antipsoriatic effect. Currently, there are few data on the pharmacokinetics of fumarates in human beings. DMF seems to act as a prodrug for its main metabolite: monomethylfumarate. This hypothesis was supported by the observation that only monomethylfumarate was detected in the plasma of human beings after the oral administration of FAEs. FAEs have been tested in different biological assays, and effects such as inhibition of the nuclear factor kappa B pathway or induction of apoptosis by DMF have been described. For these data, the role of DMF as a modulator of intracellularglutathione plays an important role.
机译：几项临床研究表明，在中度至重度牛皮癣患者中使用富马酸酯（FAE）进行全身治疗是有效的，并且具有良好的长期安全性。为了治疗用途，在德国注册了具有确定的FAE（富马酸二甲酯[DMF]和富马酸单乙酯的三种不同盐）混合物的片剂。有证据表明，DMF是该制剂中最重要的成分，具有抗银屑病作用。目前，关于富马酸酯在人体内的药代动力学的数据很少。 DMF似乎是其主要代谢产物富马酸单甲酯的前药。口服FAE后在人血浆中仅检测到富马酸单甲酯的观察结果支持了该假设。已经在不同的生物学测定中测试了FAE，并且已经描述了诸如抑制核因子Kappa B途径或DMF诱导凋亡的作用。对于这些数据，DMF作为细胞内谷胱甘肽调节剂的作用起着重要作用。

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