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[贝派地酸,新型降胆固醇药物]

[Bempedoïc acid, new cholesterol-lowering drug].

作者信息

Scheen A J, Paquot N, Wallemacq C

机构信息

Service de Diabétologie, Nutrition et Maladies métaboliques , CHU Liège, Belgique.

出版信息

Rev Med Liege. 2022 Feb;77(2):124-131.

PMID:35143133
Abstract

Patients at high or very high cardiovascular risk should have a LDL cholesterol level as low as possible, a target that may be difficult to be reached with statin monotherapy, especially when this treatment is not well tolerated. It is generally recommended to use pharmacological combinations to reach more and more strict objectives. Bempedoic acid is a new oral cholesterol-lowering medication that reduces hepatic cholesterol synthesis by inhibiting the enzyme adenosine triphosphate (ATP)-citrate lyase enzyme. Because this medication is a prodrug that is selectively activated in the liver, it is deprived of any muscular adverse effect. This article summarizes the mode of action, pharmacokinetics, efficacy, safety profile, indications and reimbursement conditions of bempedoic acid. This novel cholesterol-lowering drug is indicated in combination with statins (with or without ezetimibe) in patients who do not attain LDL goals despite administration of a statin at the maximum tolerated dose or in case of statin intolerance.

摘要

心血管风险高或极高的患者应将低密度脂蛋白胆固醇水平降至尽可能低的水平,而仅使用他汀类药物单药治疗可能难以实现这一目标,尤其是当这种治疗耐受性不佳时。一般建议使用药物联合治疗以实现越来越严格的目标。贝派地酸是一种新型口服降胆固醇药物,它通过抑制三磷酸腺苷(ATP)-柠檬酸裂解酶来减少肝脏胆固醇合成。由于这种药物是一种前体药物,在肝脏中被选择性激活,因此没有任何肌肉不良反应。本文总结了贝派地酸的作用方式、药代动力学、疗效、安全性、适应症和报销条件。这种新型降胆固醇药物适用于尽管已给予最大耐受剂量的他汀类药物但仍未达到低密度脂蛋白目标的患者,或在他汀类药物不耐受的情况下,与他汀类药物(联合或不联合依折麦布)联合使用。

相似文献

1
[Bempedoïc acid, new cholesterol-lowering drug].[贝派地酸,新型降胆固醇药物]
Rev Med Liege. 2022 Feb;77(2):124-131.
2
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.
3
Efficacy and safety of bempedoic acid in patients not receiving statins in phase 3 clinical trials.三期临床试验中,贝派地酸在未接受他汀类药物治疗患者中的疗效与安全性。
J Clin Lipidol. 2022 May-Jun;16(3):286-297. doi: 10.1016/j.jacl.2022.03.001. Epub 2022 Mar 13.
4
Bempedoic acid: Review of a novel therapy in lipid management.贝匹地酸:脂质管理中新疗法的综述。
Am J Health Syst Pharm. 2021 Jan 5;78(2):95-104. doi: 10.1093/ajhp/zxaa352.
5
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.
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.
7
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.
8
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.
9
Safety and Efficacy of Bempedoic Acid to Reduce LDL Cholesterol.贝匹地酸降低 LDL 胆固醇的安全性和有效性。
N Engl J Med. 2019 Mar 14;380(11):1022-1032. doi: 10.1056/NEJMoa1803917.
10
Efficacy and Safety of Bempedoic Acid in Patients With Hypercholesterolemia and Statin Intolerance.贝匹地酸治疗高胆固醇血症及他汀类药物不耐受患者的疗效和安全性。
J Am Heart Assoc. 2019 Apr 2;8(7):e011662. doi: 10.1161/JAHA.118.011662.