Bempedoic acid (ETC-1002) is an novel, first-in-class, orally available, once-daily low-density lipoprotein cholesterol (LDL-C) lowering small molecule designed to lower elevated levels of LDL-C and to avoid side effects associated with existing LDL-C lowering therapies. Bempedoic acid is absorbed rapidly in the small intestine and enters the liver through cell surface receptors different from those transporters that selectively take up statins.

Once in the liver, bempedoic acid inhibits ATP-citrate lyase (ACL). Pre-clinical studies show that in the liver, bempedoic acid is converted to a derivative coenzyme, or ETC-1002-CoA, which directly inhibits ACL, a key enzyme that supplies substrate for cholesterol and fatty acid synthesis in the liver.

To date, Esperion has studied bempedoic acid in ten completed clinical trials.

BEMPEDOIC ACID Phase 1 and 2 Clinical Studies**

Total Subjects: 1072 / Treated: 726Completed ETC-1002 Studies_Jan 2016

*Average LDL-C % change from baseline
**As of July 2015

Phase 2 Clinical Study Results

Our completed Phase 2 clinical studies have demonstrated significant LDL-C reductions of up to 30% as monotherapy and almost 50% in combination with ezetimibe, and consistently lower hsCRP. High sensitivity C-reactive protein, or hsCRP, is a key marker of inflammation associated with cardiovascular disease.

Across all completed clinical studies, bempedoic acid has displayed compelling, positive clinical results throughout 10 completed Phase 1 and 2 studies. To date, one serious adverse event, considered unrelated to bempedoic acid, has been observed in over 700 patients treated with bempedoic acid at doses of up to 240 mg and up to 12 weeks in duration.

Initially, we intend to seek approval of bempedoic acid for patients with elevated levels of LDL-C who are unable to tolerate statin therapy due to muscle pain or weakness. We are confident patients, physicians and payers will welcome a new, oral LDL-C lowering therapy, especially the estimated 3.5 million patients in the U.S. who are considered intolerant to statin therapy, a patient population with a high level of unmet medical need.