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Bempedoic acid - how will it shape the future lipid-lowering landscape? Mode of action, evidence, and clinical use.
Cardiology ( IF 1.9 ) Pub Date : 2023-11-21 , DOI: 10.1159/000535372
Heinz Drexel 1, 2, 3 , Arthur Mader 1, 4
Affiliation  

Background Low density lipoproteins are now proven to be causal for atherosclerosis. Pharmacological treatment focuses on an increase of LDL receptors, particularly in the hepatocyte, which leads to uptake of LDL from blood, thereby reducing the burden to the arterial wall. This mechanism has first been proven by statins to be effective to reduce cardiovascular morbidity and mortality. The concept of "the lower, the better" was shown by high-intensity statins and new compounds like ezetimibe, PCSK9-antibodies, inclisiran and ultimately bempedoic acid. Summary Although first considered only a relatively weak LDL-C lowering drug, bempedoic acid proved to be very effective for example in statin-intolerant patients to reduce cardiovascular events in the CLEAR Outcomes study. In the era of personalized medicine, it should not be forgotten, that the individual response to a LDL-C lowering drug can vary considerably. Bempedoic acid has a favorable safety profile, particularly it does not induce muscle problems because its precursor is not metabolized to the active drug in the muscle, and it does not induce hyperglycemia. Bempedoic acid probably is best used in combination with ezetimibe, which leads to LDL-C reductions in the range of moderately intensive statins; in an oral triple combination with a high-intensity statin, LDL-C reductions in the range of two thirds can be achieved. Key messages Bempedoic acid is a further weapon against the atherogenic effect of LDL cholesterol - both in primary and in secondary prevention.

中文翻译:

Bempedoic Acid——它将如何塑造未来的降脂格局?作用方式、证据和临床使用。

背景 低密度脂蛋白现已被证明是导致动脉粥样硬化的原因。药物治疗的重点是增加 LDL 受体,尤其是肝细胞中的 LDL 受体,从而导致从血液中摄取 LDL,从而减轻动脉壁的负担。这种机制首先被他汀类药物证明可以有效降低心血管发病率和死亡率。高强度他汀类药物和新化合物(如依折麦布、PCSK9 抗体、inclisiran 和最终的 bempedoic 酸)体现了“越低越好”的概念。摘要 尽管最初被认为只是一种相对较弱的 LDL-C 降低药物,但 CLEAR Outcomes 研究证明,bempedoic 酸对于他汀类药物不耐受的患者减少心血管事件非常有效。在个性化医疗时代,不应忘记,个体对降低 LDL-C 药物的反应可能存在很大差异。Bempedoic Acid 具有良好的安全性,特别是它不会引起肌肉问题,因为其前体不会在肌肉中代谢为活性药物,并且不会引起高血糖。Bempedoic Acid 可能最好与依折麦布 (ezetimibe) 联合使用,这会导致中等强度他汀类药物范围内的 LDL-C 降低;在与高强度他汀类药物的口服三联疗法中,可以实现三分之二范围内的 LDL-C 降低。关键信息 Bempedoic 酸是对抗 LDL 胆固醇造成动脉粥样硬化效应的进一步武器 - 无论是在一级预防还是二级预防中。
更新日期:2023-11-21
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