Di Giacomo-Barbagallo Francesco, Andreychuk Natalia, Scicali Roberto, Gonzalez-Lleó Ana, Piro Salvatore, Masana Lluis, Ibarretxe Daiana
Unitat de Medicina Vascular I Metabolismo, Hospital Universitario Sant Joan, Universitat Rovira I Virgili, IISPV, CIBERDEM, Reus, Spain.
Department of Clinical and Experimental Medicine, Internal Medicine, Garibaldi-Nesima Hospital, University of Catania, 95122, Catania, Italy.
Curr Atheroscler Rep. 2025 Jan 9;27(1):25. doi: 10.1007/s11883-024-01271-x.
A significant number of patients fail to achieve target LDL cholesterol (LDL-C) levels. This review aims to explore why inclisiran, a novel class of LLT, should be considered a valuable addition to the current treatment options.
Inclisiran is a small interfering RNA (siRNA) that targets PCSK9 synthesis specifically in the hepatocytes. The drug remains in circulation for less than 48 h, but its effect lasts for over six months. Two subcutaneous injections per year consistently lowers LDL-C by approximately 55% with a favorable safety profile. In combination with other LLTs, it can achieve LDL-C reductions of over 80%, supporting its role in high-intensity LLT strategies. Inclisiran represents a novel class of LLT. Administered biannually, reduces baseline LDL-C levels by half. Additionally, it has a strong safety profile. Due to its pharmacokinetic properties, is likely to improve adherence to LLT and persistently maintain low LDL-C levels.
相当一部分患者未能达到低密度脂蛋白胆固醇(LDL-C)目标水平。本综述旨在探讨为何作为一类新型降脂疗法(LLT)的inclisiran应被视为当前治疗方案中的一项有价值的补充。
Inclisiran是一种小干扰RNA(siRNA),专门靶向肝细胞中的前蛋白转化酶枯草溶菌素9(PCSK9)合成。该药物在循环系统中的停留时间不到48小时,但其效果持续超过六个月。每年两次皮下注射可使LDL-C持续降低约55%,且安全性良好。与其他降脂疗法联合使用时,它可使LDL-C降低超过80%,这支持了其在高强度降脂治疗策略中的作用。Inclisiran代表了一类新型降脂疗法。每半年给药一次,可将基线LDL-C水平降低一半。此外,它具有良好的安全性。由于其药代动力学特性,它可能会提高对降脂治疗的依从性,并持续维持较低的LDL-C水平。