Bempedoic acid is a prodrug, with an innovative mechanism that is complementary to—yet distinct from—other lipid-lowering therapies, including statins.2
Bempedoic acid is converted to its active moiety primarily in the liver, and inhibits adenosine triphosphate citrate lyase (ACL)—an enzyme two steps upstream from HMG-CoA reductase, the target of statins—along the cholesterol biosynthesis pathway.2
By inhibiting ACL, bempedoic acid reduces cholesterol synthesis, resulting in LDL receptor upregulation and increased clearance of LDL from the bloodstream.2
Bempedoic acid is converted to its active moiety by ACSVL1, which is not present in skeletal muscle. Therefore, bempedoic acid is not converted to its active moiety within skeletal muscle.2
Feb. 20, 2019
Feb. 11, 2019
Also, on February 11, 2019, Esperion submitted a Marketing Authorization Application (MAA) for an
LDL-C lowering indication for bempedoic acid 180 mg/ezetimibe 10 mg combination tablet consistent with the European Medicines Agency’s “Guideline on Clinical Development of Fixed Combination Medicinal Products.”
3. Evaluation of major cardiovascular events in patients with, or at high risk for, cardiovascular disease who are statin intolerant treated with bempedoic acid (ETC-1002) or placebo (CLEAR Outcomes). ClinicalTrials.gov. https://clinicaltrials.gov/ct2/show/NCT02993406. Accessed
February 8, 2019. 4. Evaluation of long-term safety and tolerability of ETC-1002 in high-risk patients with hyperlipidemia and high CV risk (CLEAR Harmony). ClinicalTrials.gov.
https://clinicaltrials.gov/ct2/show/NCT02666664. Accessed February 8, 2019. 5. Evaluation of the efficacy and safety of bempedoic acid (ETC-1002) in patients with hyperlipidemia
and statin intolerant (CLEAR Serenity). ClinicalTrials.gov.
https://clinicaltrials.gov/ct2/show/NCT02988115. Accessed February 8, 2019. 6. Evaluation of the efficacy and safety of bempedoic acid (ETC-1002) as add-on to ezetimibe therapy in patients with elevated LDL-C (CLEAR Tranquility). ClinicalTrials.gov. https://clinicaltrials.gov/ct2/show/NCT03001076. Accessed February 8, 2019. 7. Evaluation of long-term efficacy of bempedoic acid (ETC-1002) in patients with hyperlipidemia at high cardiovascular risk (CLEAR Wisdom). ClinicalTrials.gov. https://clinicaltrials.gov/ct2/show/NCT0299111. Accessed February 8, 2019.