LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept.

Tamer Coskun,Kyle W Sloop,Corina Loghin,Jorge Alsina-Fernandez,Shweta Urva,Krister B Bokvist,Xuewei Cui,Daniel A Briere,Over Cabrera,William C Roell,Uma Kuchibhotla,Julie S Moyers,Charles T Benson,Ruth E Gimeno,David A D'Alessio,Axel Haupt

Molecular Metabolism（2018）

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摘要

•LY3298176 activates both GIP and GLP-1 receptor signaling in vitro.•LY3298176 lowers blood glucose in mice through actions on both incretin receptors.•LY3298176 reduced fasting glucose in humans with type 2 diabetes.•Weight loss was greater with LY3298176 than the selective GLP-1 receptor agonist, dulaglutide in healthy humans.•Tolerability of LY3298176 was comparable to GLP-1 receptor agonists.

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关键词

Glucagon-like peptide-1,Glucose-dependent insulinotropic polypeptide,LY3298176,Obesity,Type 2 diabetes mellitus

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