Bardolia Chandni, Amin Nishita Shah, Turgeon Jacques
Office of Translational Research and Residency Programs, Tabula Rasa HealthCare, Moorestown, NJ, United States.
Precision Pharmacotherapy Research and Development Institute, Tabula Rasa HealthCare, Lake Nona, FL, United States.
Front Cardiovasc Med. 2021 Nov 17;8:789931. doi: 10.3389/fcvm.2021.789931. eCollection 2021.
Low-density lipoprotein cholesterol (LDL-C) is a modifiable risk factor for the development of atherosclerotic cardiovascular disease. Statins have been the gold standard for managing cholesterol levels and reducing the risks associated with atherosclerotic cardiovascular disease; however, many patients do not achieve their cholesterol goals or are unable to tolerate this drug class due to adverse drug events. Recent studies of non-statin cholesterol lowering drugs (i.e., ezetimibe, PCSK9 inhibitors) have demonstrated cardiovascular benefits; and new drugs [i.e., bempedoic acid (BDA), inclisiran] have produced promising results in pre-clinical and clinical outcome trials. This narrative review aims to discuss the place in therapy of ezetimibe, PCSK9 inhibitors, BDA, and inclisiran and describe their relative pharmacokinetic (PK) profiles, efficacy and safety as monotherapy and combination therapy, and cardiovascular benefit(s) when used for hypercholesterolemia.
低密度脂蛋白胆固醇（LDL-C）是动脉粥样硬化性心血管疾病发生的一个可改变的危险因素。他汀类药物一直是管理胆固醇水平和降低动脉粥样硬化性心血管疾病相关风险的金标准；然而，许多患者未达到其胆固醇目标，或者由于药物不良事件而无法耐受这类药物。近期对非他汀类降胆固醇药物（即依折麦布、前蛋白转化酶枯草溶菌素9型抑制剂）的研究已证明其心血管益处；并且新药[即贝派地酸（BDA）、inclisiran]在临床前和临床结局试验中已产生了有前景的结果。本叙述性综述旨在讨论依折麦布、前蛋白转化酶枯草溶菌素9型抑制剂、BDA和inclisiran在治疗中的地位，并描述它们作为单药治疗和联合治疗时相对的药代动力学（PK）特征、疗效和安全性，以及用于高胆固醇血症时的心血管益处。
