BEMPEDOIC ACID

Bempedoic acid (ETC-1002) is a 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 14 completed Phase 1 and Phase 2 clinical studies.

BEMPEDOIC ACID Phase 2 Completed Clinical Studies**

esperion-phase-2-completed-studies-103116

Total Subjects: 1045 / Treated: 810

*Average LDL-C % change from baseline (placebo corrected)
**As of October 2016

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 consistent and compelling, positive clinical results throughout 14 completed Phase 1 and 2 studies. To date, one serious adverse event, considered unrelated to bempedoic acid, has been observed in over 800 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 not adequately controlled with current lipid-modifying therapies. Some patients with elevated LDL-C are only able to tolerate less than the lowest approved daily starting dose of a statin and can be considered “statin intolerant”. We are confident patients, physicians and payers will welcome a new, oral LDL-C lowering therapy, especially the estimated 8 million patients in the U.S., Europe and Japan who are considered “statin intolerant”, a patient population with a high level of unmet medical need.