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An Update on New Cholesterol Inhibitor: Bempedoic Acid.

ABSTRACT: An increase in the level of cholesterol day by day is easily seen in most people just because of poor life style, food with high cholesterol, lack of physical work, etc. There are lots of molecules available, which lower down the cholesterol level. In this field a new molecule has been introduced that is bimpedoic acid. Researches indicate that bempedoic acid has the same mechanism of action as statins, which means that it also inhibits the HMG-CoA reductase enzyme. This article is my best collection of published scientific data on bempedoic acid till now. It also includes the chemistry, pharmacodynamic and pharmacokinetic parameters of the mentioned new molecule.

SUBMITTER: Kulshreshtha M

PROVIDER: S-EPMC9413737 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature

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An Update on New Cholesterol Inhibitor: Bempedoic Acid.

Kulshreshtha Mayank M

Current cardiology reviews 20220101 2

An increase in the level of cholesterol day by day is easily seen in most people just because of poor life style, food with high cholesterol, lack of physical work, etc. There are lots of molecules available, which lower down the cholesterol level. In this field a new molecule has been introduced that is bimpedoic acid. Researches indicate that bempedoic acid has the same mechanism of action as statins, which means that it also inhibits the HMG-CoA reductase enzyme. This article is my best colle ...[more]

PMID: 34906059

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Project description:Diabetes is a major risk factor for atherosclerotic cardiovascular disease (ASCVD) in which dyslipidaemia plays a crucial role. Statins are first line therapy for primary and secondary prevention of ASCVD; however, adverse events include reversible musculoskeletal and liver side effects in addition to a diabetogenic association. In this short review, we provide a succinct narrative of the future role and current trial data of a novel first-in-class molecule, bempedoic acid. The authors provide their expert insight with a focus on Phase III randomised controlled trials (RCT) of bempedoic acid. Bempedoic acid was approved by the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) in February and March 2020, respectively, and is a novel molecule which inhibits cholesterol biosynthesis in the same mechanistic pathway as statins. It is a first-in-class small molecule, delivered as a prodrug and administered as an oral, once-daily dose that decreases low-density lipoprotein cholesterol (LDL-C) levels. Phase II and III RCTs have demonstrated efficacy with adequate safety data as mono- or combination therapy with statins and ezetimibe. Bempedoic acid is hepatically converted to the active drug with a lack of activation in skeletal muscle. Due to this novel mechanism, musculoskeletal-related adverse events exhibit a lower prevalence providing an alternative pharmacotherapy in statin-intolerant patients. Bempedoic acid may be used as an adjunct to diet and maximally tolerated statin therapy or in statin-intolerant patients for the treatment of dyslipidaemia. The recent National Institute of Health and Care Excellence (NICE) (UK) technology appraisal guidance [TA694] published in April 2021 recommended bempedoic acid with ezetimibe as a treatment option for primary hypercholesterolaemia or mixed dyslipidaemia if statins are not tolerated or contraindicated and if there is inadequate control of LDL-C with ezetimibe alone. Additionally, outcomes trials evaluating 'hard' endpoints in statin-intolerant patients or those with ASCVD are currently underway.

Project description:Many patients do not achieve optimal low-density lipoprotein cholesterol (LDL-C) levels with statins alone; others are unable to tolerate statin therapy. Additional non-statin treatment options including ezetimibe, proprotein convertase subtilisin/kexin type 9 inhibitors, and bile acid sequestrants are often necessary to further reduce the risk of atherosclerotic cardiovascular disease. This review provides practical guidance as to the use of bempedoic acid to lower LDL-C and includes direction as to which patients may benefit and advice for safety monitoring during treatment. Bempedoic acid, a new class of agent, is a prodrug converted to bempedoyl-CoA by very long-chain acyl-CoA synthetase 1, an enzyme with high expression in the liver but that is undetectable in the skeletal muscle. Bempedoic acid inhibits the enzyme adenosine triphosphate (ATP)-citrate lyase, which lies two steps upstream from β-hydroxy β-methylglutaryl-CoA reductase in the cholesterol biosynthesis pathway. In clinical trials conducted in patients with or at risk for atherosclerotic cardiovascular disease or familial heterozygous hypercholesterolemia, bempedoic acid in combination with statins and/or ezetimibe significantly reduced LDL-C, apolipoprotein B, and high-sensitivity C-reactive protein compared with placebo. Bempedoic acid is generally well tolerated with no clinically meaningful increase in muscle-related symptoms relative to placebo, even in patients taking maximally tolerated statins. A small increase in serum uric acid (mean increase 0.8 mg/dL) is the most noteworthy adverse effect. Bempedoic acid provides an effective and generally well-tolerated medication to further reduce LDL-C in patients taking maximally tolerated statins or manage LDL-C levels in those who are unable to take statins. The potential for a reduced incidence of major cardiovascular events with bempedoic acid is being investigated in the CLEAR Outcomes trial, with results expected in 2023.

Dataset Information

An Update on New Cholesterol Inhibitor: Bempedoic Acid.

Publications

An Update on New Cholesterol Inhibitor: Bempedoic Acid.

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