作为新型小干扰RNA(small interfering RNA,siRNA)降脂药物,英克司兰于2023年8月22日在我国获批,商品名为乐可为®,该药物直接靶向递送至肝细胞,阻断前蛋白转换酶枯草溶菌素9(proprotein convertase dubtilisin/kexin type 9,PCSK9)的合成,降低血液循环中低密度脂蛋白(low-density lipoprotein,LDL-C)的水平,从而达到降脂的疗效.该药物降脂作用高效、长效且具有良好的安全性、耐受性,唯一不良反应仅为注射部位的不良事件,轻、中度肝肾功能不全患者及老年人使用该药物时也无需调整剂量,与其他降脂疗法联合用药时效果更优.本文对其作用机制、药效学、药动学、安全性评价及临床研究等进行综述.
Inclisiran:a new small interfering RNA drug for the treatment of hypercholestermia
As a new small interfering RNA(siRNA)lipid-lowering drug approved in China on August 22,2023,inclisiran(trade name"Leqvio®")is directly targeted to liver cells and blocks the synthesis of the proprotein convertase dubtilisin/kexin type 9(PCSK9),thereby reducing the level of low-density lipoprotein(LDL-C)in the blood circulation.The lipid-lowering effect of inclisiran is efficient and long-lasting,with good safety and tolerability.The only adverse reactions are adverse events at the injection site.Patients with mild and moderate hepatic and renal dysfunction and the elderly do not need to adjust dosage when using this drug,and the combination of inclisiran with other lipid-lowering therapies has a better effect.In this paper,the mechanism of action,pharmacodynamics,pharmacokinetics,safety evaluation and clinical studies of inclisiran are reviewed.
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