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Overview
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Background
ETC-1002 is an oral ACL inhibitor (IC50= 29 μM) and AMPK activator. In vitro, ETC-1002 increased levels of AMP-activated protein kinase (AMPK) phosphorylation, reduced activity of MAP kinases and decreased production of proinflammatory cytokines and chemokines. These effects on soluble mediators of inflammation can be significantly abrogated by LKB1 siRNAs, indicating that ETC-1002 activates AMPK and exerts its anti-inflammatory effects via an LKB1-dependent mechanism. [1]In vivo, ETC-1002 suppressed thioglycollate-induced homing of leukocytes into mouse peritoneal cavity. ETC-1002 restored adipose AMPK activity, reduced JNK phosphorylation, and diminished expression of macrophage-specific marker 4F/80 in a mouse model of diet-induced obesity. [1]In clinical trial, ETC-1002 reduced low-density lipoprotein-cholesterol (LDL-C) and other lipids and improved in high-sensitivity C-reactive protein in patients with type 2 diabetes mellitus and hypercholesterolemia without worsening glycemic control. ETC-1002 was low toxicity in this population. [2]
1. Filippov S1, Pinkosky SL, Lister RJ et al. ETC-1002 regulates immune response, leukocyte homing, and adipose tissue inflammation via LKB1-dependent activation of macrophage AMPK. J Lipid Res. 2013 Aug;54(8):2095-108.
2. Gutierrez MJ1, Rosenberg NL, Macdougall DE et al. Efficacy and safety of ETC-1002, a novel investigational low-density lipoprotein-cholesterol-lowering therapy for the treatment of patients with hypercholesterolemia and type 2 diabetes mellitus. Arterioscler Thromb Vasc Biol. 2014 Mar;34(3):676-83.
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