ACH-000143(ACH-000143) - 药物靶点：MTNR1A x MTNR1B_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

MTNR1A x MTNR1B

作用机制

MTNR1A激动剂(褪黑激素受体1A激动剂)、MTNR1B激动剂(褪黑激素受体1B激动剂)

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

Aché Laboratórios Farmacêuticos SA

在研机构

Aché Laboratórios Farmacêuticos SA

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)-

特殊审评-

关联

100 项与 ACH-000143 相关的临床结果

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100 项与 ACH-000143 相关的转化医学

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100 项与 ACH-000143 相关的专利（医药）

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1

项与 ACH-000143 相关的文献（医药）

2021-02-25·Journal of Medicinal Chemistry1区 · 医学

Discovery of ACH-000143: A Novel Potent and Peripherally Preferred Melatonin Receptor Agonist that Reduces Liver Triglycerides and Steatosis in Diet-Induced Obese Rats

1区 · 医学

Article

作者: Segretti, Natanael Dante ; Azevedo, Hatylas ; Russo, Elisa ; Mascarello, Alessandra ; Ferreira, Marcos Antonio ; Russo, Valter ; Guimarães, Cristiano Ruch Werneck

The modulation of melatonin signaling in peripheral tissues holds promise for treating metabolic diseases like obesity, diabetes, and nonalcoholic steatohepatitis. Here, several benzimidazole derivatives have been identified as novel agonists of the melatonin receptors MT1 and MT2. The lead compounds 10b, 15a, and 19a demonstrated subnanomolar potency at MT1/MT2 receptors, high oral bioavailability in rodents, peripherally preferred exposure, and excellent selectivity in a broad panel of targets. Two-month oral administration of 10b in high-fat diet rats led to a reduction in body weight gain similar to dapagliflozin with superior results on hepatic steatosis and triglyceride levels. An early toxicological assessment indicated that 10b (also codified as ACH-000143) was devoid of hERG binding, genotoxicity, and behavioral alterations at doses up to 100 mg/kg p.o., supporting further investigation of this compound as a drug candidate.

100 项与 ACH-000143 相关的药物交易

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