Bempedoic acid and its role in contemporary management of hyperlipidemia in atherosclerosis. [Review]
Bempedoic acid and its role in contemporary management of hyperlipidemia in atherosclerosis. [Review]
- 2022
Atherosclerotic heart disease is the leading cause of mortality and morbidity in the USA. Low density lipoprotein (LDL) has been the target for many hypolipidemic agents to modify atherosclerotic risk. Bempedoic acid is a novel hypolipidemic drug that inhibits the enzymatic activity of ATP citrate lyase in the cholesterol synthesis pathway. CLEAR Harmony, CLEAR Wisdom, CLEAR Tranquillity and CLEAR Serenity have shown safety and efficacy associated with long term administration of this drug. Studies have shown effectiveness in reducing LDL-C in both statin intolerant patients and in patients on maximally tolerated doses of statin. The fixed drug combination of bempedoic acid and ezetimibe in a recent phase III showed significant reduction in LDL compared with placebo, which might be a promising future for LDL reduction among statin intolerant patients. Bempedoic acid also reduced inflammatory markers like hs-CRP. Given these results, bempedoic acid alone and in combination with ezetimibe received the USA FDA approval for adults with heterozygous familial hypercholesterolaemia or established atherosclerotic cardiovascular disease. We present a comprehensive review exploring the underlying mechanism, pre-clinical studies, and clinical trials of bempedoic acid and discuss the potential future role of the drug in treating hyperlipidaemia.
English
0785-3890
10.1080/07853890.2022.2059559 [doi] PMC9090378 [pmc]
*Atherosclerosis
*Hydroxymethylglutaryl-CoA Reductase Inhibitors
*Hyperlipidemias
Atherosclerosis/dt [Drug Therapy]
Cholesterol, LDL
Dicarboxylic Acids
Ezetimibe/tu [Therapeutic Use]
Fatty Acids
Humans
Hydroxymethylglutaryl-CoA Reductase Inhibitors/tu [Therapeutic Use]
Hyperlipidemias/ci [Chemically Induced]
Hyperlipidemias/dt [Drug Therapy]
Hypolipidemic Agents/ae [Adverse Effects]
MedStar Heart & Vascular Institute
Journal Article
Research Support, Non-U.S. Gov't
Review
Atherosclerotic heart disease is the leading cause of mortality and morbidity in the USA. Low density lipoprotein (LDL) has been the target for many hypolipidemic agents to modify atherosclerotic risk. Bempedoic acid is a novel hypolipidemic drug that inhibits the enzymatic activity of ATP citrate lyase in the cholesterol synthesis pathway. CLEAR Harmony, CLEAR Wisdom, CLEAR Tranquillity and CLEAR Serenity have shown safety and efficacy associated with long term administration of this drug. Studies have shown effectiveness in reducing LDL-C in both statin intolerant patients and in patients on maximally tolerated doses of statin. The fixed drug combination of bempedoic acid and ezetimibe in a recent phase III showed significant reduction in LDL compared with placebo, which might be a promising future for LDL reduction among statin intolerant patients. Bempedoic acid also reduced inflammatory markers like hs-CRP. Given these results, bempedoic acid alone and in combination with ezetimibe received the USA FDA approval for adults with heterozygous familial hypercholesterolaemia or established atherosclerotic cardiovascular disease. We present a comprehensive review exploring the underlying mechanism, pre-clinical studies, and clinical trials of bempedoic acid and discuss the potential future role of the drug in treating hyperlipidaemia.
English
0785-3890
10.1080/07853890.2022.2059559 [doi] PMC9090378 [pmc]
*Atherosclerosis
*Hydroxymethylglutaryl-CoA Reductase Inhibitors
*Hyperlipidemias
Atherosclerosis/dt [Drug Therapy]
Cholesterol, LDL
Dicarboxylic Acids
Ezetimibe/tu [Therapeutic Use]
Fatty Acids
Humans
Hydroxymethylglutaryl-CoA Reductase Inhibitors/tu [Therapeutic Use]
Hyperlipidemias/ci [Chemically Induced]
Hyperlipidemias/dt [Drug Therapy]
Hypolipidemic Agents/ae [Adverse Effects]
MedStar Heart & Vascular Institute
Journal Article
Research Support, Non-U.S. Gov't
Review