DS-1150(DS-1150) - 药物靶点：GLUT-4_专利_临床

概要

基本信息

药物类型

小分子化药

别名

DS 1150、DS-1150B

靶点

GLUT-4

作用方式

刺激剂

作用机制

GLUT-4刺激剂(葡萄糖转运蛋白4 刺激剂)

治疗领域

内分泌与代谢疾病

在研适应症-

非在研适应症

2型糖尿病

原研机构

Daiichi Sankyo Co., Ltd.

在研机构-

非在研机构

Daiichi Sankyo Co., Ltd.

权益机构-

最高研发阶段无进展临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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关联

1

项与 DS-1150 相关的临床试验

NCT02004678

/ Completed临床1期

Phase I, Single-Blind, Placebo-Controlled, Randomized, Two-Part, Sequential, Single Ascending Dose Study to Assess the Safety, Pharmacokinetics and Pharmacodynamics of DS-1150b in Healthy Subjects and Subjects With Type-2 Diabetes Mellitus

DS-1150b is being developed by Daiichi Sankyo for the treatment of Type 2 Diabetes Mellitus. This is a Phase I, single-blind (subjects and principal investigator blinded, Sponsor unblinded), placebo-controlled, randomized, 2-part, sequential, single ascending dose, single center study to assess the safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral dose of DS-1150b in healthy subjects and subjects with Type 2 Diabetes Mellitus.

开始日期2013-09-01

申办/合作机构

Daiichi Sankyo Co., Ltd.

100 项与 DS-1150 相关的临床结果

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100 项与 DS-1150 相关的转化医学

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100 项与 DS-1150 相关的专利（医药）

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1

项与 DS-1150 相关的文献（医药）

2025-07-01·BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of DS-1150b, a novel xanthene compound for activating GLUT4 translocation

Article

作者: Kagechika, Katsuji ; Soneda, Tsuyoshi ; Harada, Jun ; Meguro, Masaki ; Doi, Fuminao ; Inoue, Shinichi ; Ono, Makoto ; Konishi, Masahiro ; Tanaka, Jun ; Furuzono, Shinji

The glucose transporter 4 (GLUT4) is a high-affinity glucose transporter that is predominantly expressed in the skeletal muscle, myocardium, and adipose tissue, and is the rate-limiting transporter of insulin-stimulated glucose uptake. Compounds that enhance the process of GLUT4 translocation in skeletal muscle would provide a novel treatment for type 2 diabetes mellitus. After a high-throughput screening (HTS) campaign and medicinal chemistry efforts, we identified the xanthene compound DS-1150b (16·tBuNH₂) as a novel potent GLUT4 translocation enhancer. DS-1150b was found to promote GLUT4 translocation in L6-myotubes in rats and showed a glucose-lowering effect in an oral glucose tolerance test (oGTT) in a Zucker fatty rat model. Identification of naphthalene analog DS20060511 is also briefly described.

100 项与 DS-1150 相关的药物交易

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