一种新型高效、安全的全身抗痤疮药物。

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Zouboulis CC

一种新型高效、安全的全身抗痤疮药物。

皮肤内分泌。2009五月;1(3):188-92。

PubMed ID

20436887 (PubMed视图

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摘要

组织炎症是痤疮过程的主要组成部分。白三烯B(4) (LTB(4))被认为是组织炎症发展的主要参与者。LTB(4)的合成由5-脂氧合酶控制。由于Zileuton阻断了5-脂氧合酶的活性，因此已经进行了实验和临床研究，以测试该化合物的功能模式，以及治疗寻常性痤疮的有效性和安全性。人SZ95皮脂细胞和体外炎症细胞在mRNA和蛋白质水平上表达白三烯途径的酶，参与LTB生物合成的酶在痤疮皮脂腺中被激活。用Zileuton预处理SZ95皮脂细胞部分阻止了短期花生四烯酸诱导的作用，如诱导LTB(4)，增加中性脂质含量和刺激interlekin-6释放。长期服用Zileuton可直接降低SZ95 seb细胞中性脂质的含量和白细胞介素-6的释放。PPAR mRNA水平不受Zileuton的调控。在一项针对10名丘疹性痤疮患者的初步临床研究中，Zileuton 4 x 600 mg/d p.o.连续3个月以时间依赖方式降低了痤疮严重程度指数，在第12周时降低了初始评分的41% (p < 0.05)。这主要是由于炎症病变数量减少了29% (p < 0.01)。 In addition, total sebum lipids significantly decreased (35%, p < 0.05) and the pro-inflammatory free fatty acids (22%) and lipoperoxides (26%) were markedly diminished in patients' sebum under treatment. The magnitude of clinical improvement strongly correlated with the reduction of total sebum lipids (p = 0.0009, r(2) = 0.81) and free fatty acids (p = 0.0003, r(2) = 0.82). In a further study, a 40-year-old female with mild disseminated sebaceous gland hyperplasia and seborrhea, responded with normalization of the casual skin surface lipids and similar reduction of facial sebum synthesis under treatment with Zileuton over 2weeks and-after a wash-out phase-low-dose isotretinoin (10 mg/2nd d) over 5 weeks. These data are in agreement with a phase II multicenter, clinical study in 101 patients with mild to moderate inflammatory facial acne conducted in the US, which showed a significant efficacy of Zileuton in a subset of patients with moderate acne, whereas those patients treated with Zileuton showed a significant mean decrease in inflammatory lesions compared to the placebo group. In all clinical studies, Zileuton was found to be safe and well tolerated.

引用本文的药物库数据

药物靶点

药物	目标	种类	生物	药理作用	行动
食品与	花生四烯酸5-lipoxygenase	蛋白质	人类	是的	抑制剂	细节