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贝匹地酸:一种具有新型作用机制的降胆固醇药物。

Bempedoic Acid: a cholesterol lowering agent with a novel mechanism of action.

机构信息

Department of Clinical Sciences, The Ben and Maytee Fisch College of Pharmacy, Texas, USA.

出版信息

Expert Rev Clin Pharmacol. 2021 May;14(5):545-551. doi: 10.1080/17512433.2021.1901579. Epub 2021 Mar 18.

DOI:10.1080/17512433.2021.1901579
PMID:33691561
Abstract

INTRODUCTION

Dyslipidemia is a common condition that increases the risk of heart diseases and stroke. High levels of low-density lipoprotein-cholesterol (LDL-C) are correlated with a higher risk for heart disease. A drug class known as 'statins' is the gold standard for LDL-C-lowering, but its use in some patients is limited by its adverse effects of myalgias and myopathies. Use of other LDL-C-lowering agents is frequently limited by cost and degree of efficacy. Additionally, many high-risk atherosclerotic cardiovascular disease patients fail to meet LDL-C goals despite maximally tolerated statin therapy with or without the addition of a non-statin agent.

AREAS COVERED

This review covers the pharmacology, pharmacokinetics, clinical trials, and clinical implications of bempedoic acid. A PubMed search was conducted using the terms bempedoic, bempedoic acid, Nexletol, ETC-1002, and adenosine triphosphate citrate lyase inhibitor. Additional data were obtained from the prescribing information and relevant guidelines. All clinical trials were included.

EXPERT OPINION

Bempedoic acid has not been shown to cause myalgias or myopathies and is likely to be competitively affordable compared to other LDL-C-lowering agents. Bempedoic acid has been shown to be superior compared to placebo and provides additional LDL-C lowering on top of maximally tolerated statin therapy or combined with ezetimibe alone.

摘要

简介

血脂异常是一种常见病症,会增加患心脏病和中风的风险。低密度脂蛋白胆固醇(LDL-C)水平升高与心脏病风险增加相关。一类名为“他汀类药物”的药物是降低 LDL-C 的金标准,但由于其肌痛和肌病的副作用,在某些患者中的使用受到限制。其他 LDL-C 降低剂的使用通常受到成本和疗效程度的限制。此外,尽管最大耐受剂量的他汀类药物治疗或联合使用非他汀类药物,许多高危动脉粥样硬化性心血管疾病患者仍未能达到 LDL-C 目标。

涵盖的领域

这篇综述涵盖了贝美前列素的药理学、药代动力学、临床试验和临床意义。使用了 bempedoic、bempedoic acid、Nexletol、ETC-1002 和三磷酸腺苷柠檬酸裂解酶抑制剂等术语在 PubMed 上进行了搜索。还从处方信息和相关指南中获取了其他数据。所有临床试验均被纳入。

专家意见

贝美前列素不会引起肌痛或肌病,与其他 LDL-C 降低剂相比,它可能更具竞争力。与安慰剂相比,贝美前列素显示出优越性,在最大耐受剂量的他汀类药物治疗或与依折麦布联合使用的基础上,还能进一步降低 LDL-C。

相似文献

1
Bempedoic Acid: a cholesterol lowering agent with a novel mechanism of action.贝匹地酸:一种具有新型作用机制的降胆固醇药物。
Expert Rev Clin Pharmacol. 2021 May;14(5):545-551. doi: 10.1080/17512433.2021.1901579. Epub 2021 Mar 18.
2
Evaluating pharmacokinetics of bempedoic acid in the treatment of hypercholesterolemia.评估贝匹地酸治疗高胆固醇血症的药代动力学。
Expert Opin Drug Metab Toxicol. 2021 Sep;17(9):1031-1038. doi: 10.1080/17425255.2021.1951222. Epub 2021 Jul 15.
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Bempedoic Acid in the Treatment of Patients with Dyslipidemias and Statin Intolerance.贝匹地酸治疗血脂异常和他汀不耐受患者。
Cardiovasc Drugs Ther. 2021 Aug;35(4):841-852. doi: 10.1007/s10557-020-07139-x. Epub 2021 Jan 27.
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Bempedoic acid. Mechanism of action and pharmacokinetic and pharmacodynamic properties.贝匹地酸。作用机制及药代动力学和药效学特性。
Clin Investig Arterioscler. 2021 May;33 Suppl 1:53-57. doi: 10.1016/j.arteri.2021.02.012.
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Bempedoic acid plus ezetimibe fixed-dose combination in patients with hypercholesterolemia and high CVD risk treated with maximally tolerated statin therapy.贝特帕酸联合依折麦布固定剂量复方制剂在最大耐受他汀治疗的高胆固醇血症和高 CVD 风险患者中的应用。
Eur J Prev Cardiol. 2020 Apr;27(6):593-603. doi: 10.1177/2047487319864671. Epub 2019 Jul 29.
6
Efficacy and safety of bempedoic acid added to ezetimibe in statin-intolerant patients with hypercholesterolemia: A randomized, placebo-controlled study.在不能耐受他汀类药物的高胆固醇血症患者中,添加苯扎贝特酸与依折麦布联合治疗的疗效和安全性:一项随机、安慰剂对照研究。
Atherosclerosis. 2018 Oct;277:195-203. doi: 10.1016/j.atherosclerosis.2018.06.002. Epub 2018 Jun 12.
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Role of Bempedoic Acid in Clinical Practice.贝匹地酸在临床实践中的作用。
Cardiovasc Drugs Ther. 2021 Aug;35(4):853-864. doi: 10.1007/s10557-021-07147-5. Epub 2021 Apr 5.
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Bempedoic acid, an inhibitor of ATP citrate lyase for the treatment of hypercholesterolemia: early indications and potential.贝派地酸,一种用于治疗高胆固醇血症的ATP柠檬酸裂解酶抑制剂:早期迹象与潜力
Expert Opin Investig Drugs. 2020 Aug;29(8):763-770. doi: 10.1080/13543784.2020.1778668. Epub 2020 Jun 21.
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Role of Bempedoic Acid in Dyslipidemia Management.贝匹地酸在血脂异常管理中的作用。
J Cardiovasc Pharmacol. 2020 Oct;76(4):376-388. doi: 10.1097/FJC.0000000000000887.
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Association of Bempedoic Acid Administration With Atherogenic Lipid Levels in Phase 3 Randomized Clinical Trials of Patients With Hypercholesterolemia.贝匹地酸治疗对高胆固醇血症患者的 3 期随机临床试验中致动脉粥样硬化脂质水平的影响。
JAMA Cardiol. 2020 Oct 1;5(10):1124-1135. doi: 10.1001/jamacardio.2020.2314.

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