Kosmas Constantine E, Muñoz Estrella Alba, Skavdis Andreas, Peña Genao Edilberto, Martinez Ian, Guzman Eliscer
Department of Medicine, Division of Cardiology, Montefiore Medical Center, Bronx, NY, USA.
Department of Medicine, Mount Sinai St. Luke's-West Hospital, New York, NY, USA.
Ther Clin Risk Manag. 2020 Oct 28;16:1031-1037. doi: 10.2147/TCRM.S230592. eCollection 2020.
Proprotein convertase subtilisin kexin 9 (PCSK-9)-targeting therapy has arisen as a new line for the treatment of hyperlipidemia. Inclisiran is a double-stranded small RNA molecule that works by blocking the transcription of PCSK-9, leading to a reduction of PCSK9 levels in the hepatocytes, resulting in an increased expression of low-density lipoprotein (LDL) receptors in the hepatocyte membrane and, as a consequence, it reduces the circulating levels of LDL cholesterol (LDL-C). Compared to the other LDL-C-lowering medications, such as statins, ezetimibe and PCSK-9 inhibitors, inclisiran proposes an infrequent dosing of twice a year, while simultaneously providing a significant reduction of LDL-C. Its prolonged effect offers an advantage against medication non-compliance, which is one of the main causes for not achieving LDL-C goals with standard therapy. Inclisiran has also proven to have a relatively safe profile with adverse effects occurring in similar frequency as with placebo. This review aims to present and discuss the current clinical and scientific data pertaining to the role of inclisiran in the management of hypercholesterolemia and treatment of cardiovascular disease (CVD).
靶向前蛋白转化酶枯草溶菌素9（PCSK-9）的疗法已成为治疗高脂血症的新途径。英克西兰是一种双链小RNA分子，其作用机制是阻断PCSK-9的转录，导致肝细胞中PCSK9水平降低，从而使肝细胞膜上低密度脂蛋白（LDL）受体的表达增加，结果是降低了循环中的低密度脂蛋白胆固醇（LDL-C）水平。与其他降低LDL-C的药物（如他汀类药物、依折麦布和PCSK-9抑制剂）相比，英克西兰建议每年给药两次，频率较低，同时能显著降低LDL-C。其长效作用有利于解决药物依从性问题，而药物依从性不佳是标准治疗无法实现LDL-C目标的主要原因之一。英克西兰还被证明具有相对安全的特性，其不良反应发生频率与安慰剂相似。本综述旨在介绍和讨论目前与英克西兰在高胆固醇血症管理和心血管疾病（CVD）治疗中的作用相关的临床和科学数据。
