Department of Pharmacotherapy and Translational Research, Colleges of Pharmacy and Medicine, University of Florida, Gainesville, FL, USA.
Department of Pharmacotherapy and Translational Research, and the Department of Community Health and Family Medicine, Colleges of Pharmacy and Medicine, University of Florida, Gainesville, FL, USA.
Clin Ther. 2021 Feb;43(2):410-420. doi: 10.1016/j.clinthera.2020.12.001. Epub 2020 Dec 29.
This article discusses the pharmacology of bempedoic acid, the trials that led to United States Food and Drug Administration (FDA) approval of its use, and the overall safety and efficacy of this therapy in heterozygous familial hypercholesterolemia, established atherosclerotic cardiovascular disease (ASCVD), and hyperlipidemia.
A database search of PubMed and ClinicalTrials.gov was conducted for articles published between January 2012 to September 2020 and containing the key words bempedoic acid, ezetimibe, Nexletol and Nexlizet. Trials from the CLEAR series were selected, as they played a pivotal role in the establishment of FDA approval, along with additional trials published after FDA approval, which provided novel evidence on the use of bempedoic acid in the treatment of hypercholesterolemia. Publications that were not randomized, controlled trials were not included in this review. Only randomized controlled trials in which ezetimibe was used in conjunction with bempedoic acid were included in this review as they were relevant to the new FDA approval of bempedoic acid.
The findings of the present review show that bempedoic acid is both an effective and well-tolerated option for the treatment of hypercholesterolemia when used without ezetimibe in addition to standard therapy. It also appears that the combination with ezetimibe increases the cholesterol-lowering effect more than either agent alone when added to standard therapy.
Hypercholesteremia continues to be a major contributing factor leading to ASCVD. Bempedoic acid is an additional treatment option, along with both statins and diet and exercise, for reducing cholesterol levels and ASCVD events. With the new FDA approval, bempedoic acid may offer an effective therapy for reducing low-density lipoprotein cholesterol in patients at high risk for cardiovascular events due to established ASCVD or heterozygous familial hypercholesterolemia.
本文讨论了贝匹达酸的药理学，导致美国食品和药物管理局（FDA）批准其使用的试验，以及在杂合家族性高胆固醇血症、已确立的动脉粥样硬化性心血管疾病（ASCVD）和血脂异常中使用这种治疗的总体安全性和疗效。
对 2012 年 1 月至 2020 年 9 月期间发表的包含贝匹达酸、依折麦布、Nexletol 和 Nexlizet 关键词的 PubMed 和 ClinicalTrials.gov 数据库进行了检索。选择了 CLEAR 系列试验，因为它们在 FDA 批准的确立中发挥了关键作用，此外，在 FDA 批准后发表的其他试验也提供了贝匹达酸在治疗高胆固醇血症中的新证据。本综述未纳入非随机对照试验的出版物。本综述仅纳入了与贝匹达酸新的 FDA 批准相关的、联合使用依折麦布的随机对照试验，因为这些试验与贝匹达酸的新 FDA 批准相关。
本综述的结果表明，贝匹达酸在联合标准治疗时，即使不联合依折麦布，也可有效且耐受良好地治疗高胆固醇血症。此外，与单独使用任一药物相比，联合使用依折麦布可进一步增强降胆固醇作用。
高胆固醇血症仍然是导致 ASCVD 的主要致病因素之一。贝匹达酸是一种额外的治疗选择，与他汀类药物、饮食和运动一起，可降低胆固醇水平和 ASCVD 事件。随着新的 FDA 批准，贝匹达酸可能为患有已确立的 ASCVD 或杂合家族性高胆固醇血症的高危心血管事件患者提供一种有效的降低低密度脂蛋白胆固醇的治疗方法。
