ETC-1002 works as an AMPK activator. ETC-1002 at 100μM increased levels of AMPK phosphorylation in primary human MDMs exposure to LPS, and decreased production of proinflammatory cytokines and chemokines. In dyslipidemic subjects, ETC-1002 not only reduces plasma LDL cholesterol but also significantly attenuates levels of hsCRP, a clinical biomarker of inflammation. Silencing of LKB1 by siRNA could significantly abrogate AMPK phosphorylation and inhibitory effects of ETC-1002 on soluble mediators of inflammation. ETC-1002 suppressed thioglycollate-induced homing of leukocytes into mouse peritoneal cavity in vivo. Also, it restored adipose AMPK activity, reduced JNK phosphorylation, and diminished expression of macrophage-specific marker 4F/80 in a mouse model of diet-induced obesity. ETC-1002 is an investigational drug currently in Phase 2 development for treatment of dyslipidemia and other cardiometabolic risk factors[2].
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