Debio 0930

Debio 0930 (also known as MT-63-78) is a novel, orally bioavailable, small-molecule direct activator of AMP-activated protein kinase (AMPK). It was originally developed by Mercury Therapeutics and licensed to Debiopharm for the treatment of type 2 diabetes and other metabolic disorders. Debio 0930 acts as a direct allosteric activator of AMPK, specifically targeting complexes containing the AMPK-beta-1 subunit (such as alpha-1-beta-1-gamma-1 heterotrimers) at the allosteric drug and metabolite (ADaM) site. In addition to allosteric activation, it protects AMPK from dephosphorylation at Thr172. Preclinical studies have demonstrated that Debio 0930 improves glycemic control, reduces hepatic glucose production, and ameliorates insulin resistance and lipid profiles in metabolic disease models [1.1]. It has also been investigated for its potential anti-tumor effects, particularly in prostate cancer, where it inhibits lipogenesis and the mTORC1 pathway, leading to mitotic arrest and apoptosis. However, development of the compound was discontinued following the cessation of operations by Mercury Therapeutics.

Other names

5-(2',6'-dihydroxy-[1,1'-biphenyl]-4-yl)-1H-indole-3-carbonitrile