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新型长效 RNA 治疗药物依洛司他仑抑制前蛋白转化酶枯草溶菌素 9 的有效性和安全性。

Effectiveness and Safety of Inclisiran, A Novel Long-Acting RNA Therapeutic Inhibitor of Proprotein Convertase Subtilisin/Kexin 9.

机构信息

Dept of Cardiology, Christian Medical College, Vellore, India.

Department of Internal Medicine, Mount Sinai St Luke's Roosevelt Hospital, Icahn School of Medicine at Mount Sinai, New York.

出版信息

Am J Cardiol. 2018 Oct 1;122(7):1272-1277. doi: 10.1016/j.amjcard.2018.06.023. Epub 2018 Jul 3.

DOI:10.1016/j.amjcard.2018.06.023
PMID:30075894
Abstract

Low-density cholesterol (LDL-C) has a causal association with coronary artery disease and acute coronary syndromes (ACS). Statins have been found to reduce LDL-C, and many randomized trials have documented the significant role of statins in prevention and treatment of ACS. Treatment with statin therapy is associated with few shortcomings. A healthy percentage of patients initiated on statin, discontinue it within a year of initiation predominantly because of its daily dosing schedule. There is considerable variability in treatment response to statins and in some percentage of patients with high risk for ACS, satins are not enough to help reach the LDL-C goal necessitating the development of alternate LDL-C lowering therapies. Inclisiran a small interfering ribonucleic acid molecule inhibitor is helpful in sustained reduction of LDL-C. A single dose can decrease LDL-C for around 6 months, showed promising results in the phase II trials. In conclusion, here we reviewed the possibilities of Inclisiran as LDL-C reducing therapy and compared with currently available newer nonstatin LDL-C lowering therapies.

摘要

低密度脂蛋白胆固醇(LDL-C)与冠状动脉疾病和急性冠状动脉综合征(ACS)有因果关系。他汀类药物已被发现可降低 LDL-C,许多随机试验也证明了他汀类药物在 ACS 的预防和治疗中的重要作用。他汀类药物治疗的缺点很少。开始接受他汀类药物治疗的健康患者中有很大一部分在开始治疗后的一年内停止治疗,主要是因为其每日剂量方案。他汀类药物治疗的反应存在相当大的差异,对于某些 ACS 高危患者,他汀类药物不足以帮助达到 LDL-C 目标,因此需要开发替代 LDL-C 降低疗法。Inclisiran 是一种小干扰核糖核酸分子抑制剂,有助于持续降低 LDL-C。一剂可降低 LDL-C 约 6 个月,在 II 期试验中显示出有前途的结果。总之,我们在这里回顾了 Inclisiran 作为 LDL-C 降低治疗的可能性,并与目前可用的新型非他汀类 LDL-C 降低治疗进行了比较。

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