与,一个新的高效、安全的系统性嫩肤药物。

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Zouboulis CC

与,一个新的高效、安全的系统性嫩肤药物。

Dermatoendocrinol。2009; 1 (3): 188 - 92。

PubMed ID

20436887 (在PubMed

]

文摘

痤疮的组织炎症是一个主要组件的过程。白三烯B (4) (LTB(4))被认为是发展的一个主要玩家组织炎症。合成的LTB(4)由酶5-lipoxygenase控制。5-lipoxygenase与街区活动以来,实验和临床研究已经进行了测试模式的功能,以及疗效和安全性的复合治疗寻常痤疮。人类SZ95架构和炎性细胞在体外表达白三烯途径的酶在信使rna和蛋白质水平和酶生物合成的LTB(4)被激活的皮脂腺痤疮病变。预处理的SZ95架构及与部分避免短期花生四烯酸段的影响,如诱导LTB(4),增加了中性脂质interlekin-6发布的内容和刺激。长期治疗与直接减少中性脂质和白细胞介素- 6的内容释放SZ95 seb ocytes。PPAR mRNA水平不是由食品与监管。在第一次试验临床研究10 papulopustular痤疮患者与4 x 600 mg / d以上规格为3个月时间的方式减少痤疮严重程度指数在第12周的初始分数的41% (p < 0.05)。这主要是由于炎症病变的数量减少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.

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药物靶点

药物	目标	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