Bempedoic Acid (ETC-1002): an Investigational Inhibitor of ATP Citrate Lyase.

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Bilen O, Ballantyne CM

Bempedoic Acid (ETC-1002): an Investigational Inhibitor of ATP Citrate Lyase.

Curr Atheroscler Rep. 2016 Oct;18(10):61. doi: 10.1007/s11883-016-0611-4.

PubMed ID

27663902 [ View in PubMed

]

Abstract

Bempedoic acid (ETC-1002), a novel therapeutic approach for low-density lipoprotein cholesterol (LDL-C) lowering, inhibits ATP citrate lyase (ACL), an enzyme involved in fatty acid and cholesterol synthesis. Although rodent studies suggested potential effects of ACL inhibition on both fatty acid and cholesterol synthesis, studies in humans show an effect only on cholesterol synthesis. In phase 2 studies, ETC-1002 reduced LDL-C as monotherapy, combined with ezetimibe, and added to statin therapy, with LDL-C lowering most pronounced when ETC-1002 was combined with ezetimibe in patients who cannot tolerate statins. Whether clinically relevant favorable effects on other cardiometabolic risk factors such as hyperglycemia and insulin resistance occur in humans is unknown and requires further investigation. Promising phase 2 results have led to the design of a large phase 3 program to gain more information on efficacy and safety of ETC-1002 in combination with statins and when added to ezetimibe in statin-intolerant patients.

DrugBank Data that Cites this Article

Drugs

Bempedoic acid

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Bempedoic acid	ATP-citrate synthase	Protein	Humans	Yes	Inhibitor	Details

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Bempedoic acid	NUAK family SNF1-like kinase 2	Protein	Humans	Unknown	Activator	Details