Bempedoic acid (ETC-1002) is an innovative, first-in-class, orally available, once-daily 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 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**
*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, 24% incremental LDL-C reduction on top of statins, 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 been well-tolerated. To date, one serious adverse event, considered unrelated to bempedoic acid, has been observed in 726 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. Subsequently, we expect that we will seek approval of bempedoic acid as an add-on to a statin in a broader population of patients who are unable to achieve their LDL-C goals, despite being on a statin regimen and therefore remain at an increased risk for cardiovascular disease. We believe bempedoic acid could provide a major contribution to reducing risk associated with elevated LDL-C by meeting the unmet needs of millions of patients.