Korea Institute of Dermatological Science, GeneCellPharm Corporation, 375 Munjeong 2(i)-dong, Songpa-gu, Seoul, 05836, South Korea.
Research Institute for Molecular-Targeted Drugs, Department of Cosmetics Engineering, Konkuk University, Seoul, 05029, South Korea.
Sci Rep. 2020 Mar 11;10(1):4493. doi: 10.1038/s41598-020-61424-1.
Nintedanib, a receptor tyrosine kinase (RTK) inhibitor has been developed as therapeutics for idiopathic pulmonary fibrosis and non-small lung cancer. We found that the expression levels of RTK, especially VEGFR1 is increased in skin biopsies of dermatitis patients from multiple independent datasets. Moreover, VEGFR1 is highly expressed by infiltrated cells in dermis from oxazolone (OXA) treated mice. Interestingly, nintedanib alleviates dermatitis symptom in OXA-induced animal model. Especially, levels of epidermis thickness, infiltrated immune cells including mast cells and eosinophils were decreased from mice cotreated with nintedanib and OXA compared with OXA treated mice. Moreover, serum IgE and Th2 cytokines including IL-4 and IL-13 were decreased by nintedanib treatment. These results suggest an evidence that nintedanib alleviates animal model of dermatitis.
尼达尼布是一种受体酪氨酸激酶(RTK)抑制剂,已被开发为特发性肺纤维化和非小细胞肺癌的治疗药物。我们发现,来自多个独立数据集的皮炎患者皮肤活检中 RTK 的表达水平,特别是 VEGFR1 的表达水平升高。此外,奥沙酮(OXA)处理的小鼠真皮中的浸润细胞高度表达 VEGFR1。有趣的是,尼达尼布可缓解 OXA 诱导的动物模型中的皮炎症状。特别是,与仅用 OXA 处理的小鼠相比,用尼达尼布和 OXA 共同处理的小鼠的表皮厚度、浸润的免疫细胞(包括肥大细胞和嗜酸性粒细胞)水平降低。此外,尼达尼布治疗还降低了血清 IgE 和 Th2 细胞因子(包括 IL-4 和 IL-13)的水平。这些结果表明,尼达尼布可缓解皮炎动物模型。