凋亡信号调节激酶1抑制剂selonsertib

An apoptosis signal regulates kinase 1 inhibitor: selonsertib

selonsertib是ASK1抑制剂,用于治疗非酒精性脂肪肝炎和酒精性肝炎,在鼠肝纤维化模型中,该抑制剂可以降低肝胶原和血清。在鼠非酒精性脂肪性肝炎模型中,selonsertib可以抑制纤维化、脂肪变性和胶原蛋白的产生,抑制羟脯氨酸的合成。口服给药后,通过抑制ASK1依赖性的信号转导通路的激活,阻止炎性细胞因子的生成、下调参与纤维化过程的基因表达、抑制过度凋亡、细胞增殖。在肝脏疾病多个评价指标方面均表现出明显改善,selonsertib是目前研究最多的ASK1抑制剂,也是先期进入临床研究阶段的药物。多项临床研究表明,selonsertib可以单独用药,也可以与其他药物联合使用,具有安全性和有效性。

selonsertib is an ASK1 inhibitor, used to treat non-alcoholic fatty hepatitis and alcoholic hepatitis. In the rat liver fibrosis model, this inhibitor reduces liver collagen and serum. In the rat model of non-alcoholic fatty hepatitis, the production of fibrosis, fatty degeneration and collagen was inhibited, and the synthesis of hydroxyproline was inhibited. After oral administration, selonsertib prevents the generation of inflammatory cytokines, reduces the gene expression involved in the fibrosis process, inhibits excessive apoptosis, and cell proliferation by inhibiting the activation of the signal transduction pathway dependent on ASK1. selonsertib is the most studied ASK1 inhibitor, and it is also a drug that has entered the clinical research stage in advance. A number of clinical studies have shown that selonsertib can be used alone or in combination with other drugs, which is safe and effective.