East Coast Institute for Research, Jacksonville, FL, USA.
University of Florida College of Pharmacy, Jacksonville, FL, USA.
Am J Cardiovasc Drugs. 2020 Dec;20(6):535-548. doi: 10.1007/s40256-020-00399-w.
Despite the widespread use of statins and ezetimibe to decrease low-density lipoprotein cholesterol (LDL-C) levels and associated atherosclerotic cardiovascular disease (ASCVD), many patients do not achieve adequate LDL-C lowering as per the recommended American College of Cardiology (ACC)/American Heart Association (AHA) and European Society of Cardiology (ESC)/European Atherosclerosis Society (EAS) guidelines and demonstrate residual cardiovascular risk. The introduction of proprotein convertase subtilisin/kexin type 9 (PCSK-9) inhibitors in 2015 was a promising addition to hypercholesterolemia therapies, but their cost and subcutaneous administration has limited their use, and therefore, new affordable and patient friendly treatment strategies are crucial to help reduce ASCVD risk. Bempedoic acid, a drug currently under investigation, is a small molecule that has been shown to upregulate LDL receptors, decrease LDL-C, and reduce atherosclerotic plaque formation in hypercholesterolemic patients. Furthermore, bempedoic acid is a prodrug that becomes activated by an enzyme expressed primarily in the liver, allowing it to avoid the potential myotoxicity associated with statin therapy. The purpose of this review is to summarize the major clinical studies evaluating bempedoic acid and describe its potential addition to currently approved lipid-lowering therapies.
尽管广泛使用他汀类药物和依折麦布来降低低密度脂蛋白胆固醇 (LDL-C) 水平并降低相关的动脉粥样硬化性心血管疾病 (ASCVD)，但许多患者并未按照美国心脏病学会 (ACC)/美国心脏协会 (AHA) 和欧洲心脏病学会 (ESC)/欧洲动脉粥样硬化学会 (EAS) 建议的指南充分降低 LDL-C，仍存在残余心血管风险。2015 年，前蛋白转化酶枯草溶菌素 9 (PCSK-9) 抑制剂的问世为高胆固醇血症治疗带来了新的希望，但由于其成本和皮下给药限制了其应用，因此，开发新的、负担得起的、适合患者的治疗策略对于降低 ASCVD 风险至关重要。目前正在研究的小分子药物苯扎贝特酸可以上调 LDL 受体，降低 LDL-C，并减少高胆固醇血症患者的动脉粥样硬化斑块形成。此外，苯扎贝特酸是一种前药，可被主要在肝脏中表达的酶激活，从而避免与他汀类药物治疗相关的潜在肌肉毒性。本文旨在总结评估苯扎贝特酸的主要临床研究，并描述其作为目前批准的降脂治疗方法的潜在补充。
