干扰小RNA抗高血压药Zilebesiran的研究进展  

Small Interfering RNA Antihypertensive Drug Zilebesiran

作　　者：关芳 康雅隆 谭娟娟 齐鸿飞 秦墁 王若楠 王海芳 GUAN Fang;KANG Yalong;TAN Juanjuan;QI Hongfei;QIN Man;WANG Ruonan;WANG Haifang(Shaanxi University of Chinese Medicine,Shaanxi Province and Xianyang Key Laboratory of Integrative Traditional Chinese and Western Medicine for the Prevention and Treatment of Cardiovascular Diseases,Xianyang 712000,Shaanxi,China)

机构地区：[1]陕西中医药大学陕西省及咸阳市中西医结合心血管病防治重点实验室,陕西咸阳712000

出　　处：《心血管病学进展》2024年第12期1099-1104,共6页Advances in Cardiovascular Diseases

基　　金：陕西省感染与免疫疾病重点实验室开放课题(2022-ZD-3);陕西省教育厅科研计划重点实验室项目(22JS006);陕西省科技厅自然科学基础研究计划一般项目(2023-JC-QN-0853);咸阳市中西医结合防治炎性疾病研究科技创新团队(L2022CXNLTD003)。

摘　　要：高血压是心脑血管疾病的重要危险因素之一。目前中国的高血压发病率高,但知晓率、诊断率、治疗率相对较低。高血压发病机制复杂,尚不完全清楚,且具有较大的个体差异性。西医治疗以口服抗高血压药为主要手段,用药间隔时间短、患者依从性差,部分患者联合用药后血压控制仍欠佳。zilebesiran是一类新型、尚处于临床研究阶段的干扰小RNA抗高血压药,能够特异性阻断肝脏血管紧张素原信使RNA的表达,从而减少肝脏血管紧张素原的合成,实现降压目的。该药物的作用靶点较传统抗高血压药更为上游,效果更为全面、强效,且半衰期长,用药频次明显减低,当前研究结果提示其短期应用具有良好的耐受性及安全性。现旨在介绍zilebesiran的作用机制和临床试验的初步结果,包括疗效及安全性,以期提高国内相关领域研究人员对该药的全面深入认识。Hypertension is one of the important risk factors of cardiovascular and cerebrovascular diseases.At present,the incidence rate of hypertension in China is high,while the awareness rate,diagnosis rate and treatment rate are relatively low.The pathogenesis of hypertension is complex,not fully understood,and has significant individual differences.Oral antihypertensive drugs are the main treatment method in Western medicine,with short medication intervals and poor compliance.Blood pressure control is still not enough in some patients after combination therapy.Zilebesiran is a new type of small interfering RNA antihypertensive drug that is still in the clinical research stage.It is proposed to specifically prevent the gene expression of liver angiotensinogen messenger RNA,thereby reducing the synthesis of angiotensinogen and achieving antihypertensive goals.The drug acts at a upstream site of traditional antihypertensive drugs,with a more comprehensive and potent effect,long half-life,and significantly reduced frequency of dosing.Current research findings suggest that its short-term use has good tolerability and safety.The aim is to introduce the mechanism of action and the preliminary results of clinical trials of zilebesiran,including its efficacy and safety,in order to enhance the comprehensive understanding of this drug among researchers in relevant fields in China.

关 键 词：Zilebesiran 高血压 干扰小RNA 血管紧张素原 

分 类 号：R544.1[医药卫生—心血管疾病]