ZLY-28(ZLY-28) - 药物靶点：FABP1 x FXR_在研适应症：代谢功能障碍相关的脂肪肝病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

FABP1 x FXR

作用机制

FABP1抑制剂(fatty acid binding protein 1 inhibitors)、FXR调节剂(胆汁酸受体FXR调节剂)

治疗领域

消化系统疾病

在研适应症

代谢功能障碍相关的脂肪肝病

非在研适应症-

原研机构

广东药科大学

在研机构

广东药科大学

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)临床前

特殊审评-

关联

100 项与 ZLY-28 相关的临床结果

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100 项与 ZLY-28 相关的转化医学

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100 项与 ZLY-28 相关的专利（医药）

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1

项与 ZLY-28 相关的文献（医药）

2023-05-11·Journal of medicinal chemistry1区 · 医学

Discovery of the First-in-Class Intestinal Restricted FXR and FABP1 Dual Modulator ZLY28 for the Treatment of Nonalcoholic Fatty Liver Disease.

1区 · 医学

Article

作者: Chen, Ya ; Cao, Zhijun ; Wang, Wenxin ; Jiao, Shixuan ; Chen, Siliang ; Huang, Wanqiu ; Cai, Zongyu ; Hu, Lijun ; Deng, Liming ; Ren, Qiang ; Li, Zheng ; Zhou, Zongtao ; Yang, Zhongcheng ; Zhang, Luyong ; Wang, Bin

The prevalence of nonalcoholic steatohepatitis (NASH) is increasing rapidly worldwide, and NASH has become a serious problem for human health. Recently, the selective activation of the intestinal farnesoid X receptor (FXR) was considered as a more promising strategy for the treatment of NASH with lesser side effects due to reduced systemic exposure. Moreover, the inhibition of intestinal fatty acid binding protein 1 (FABP1) alleviated obesity and NASH by reducing dietary fatty acid uptake. In this study, the first-in-class intestinal restricted FXR and FABP1 dual-target modulator ZLY28 was discovered by comprehensive multiparameter optimization studies. The reduced systemic exposure of ZLY28 might provide better safety by decreasing the on- and off-target side effects in vivo. In NASH mice, ZLY28 exerted robust anti-NASH effects by inhibiting FABP1 and activating the FXR-FGF15 signaling pathway in the ileum. With the above attractive efficacy and preliminary safety profiles, ZLY28 is worthy of further evaluation as a novel anti-NASH agent.

100 项与 ZLY-28 相关的药物交易

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