Drugs reducing plasma concentrations of apolipoprotein B–containing lipoproteins have been demonstrated to reduce the risk of cardiovascular disease (CVD) in both primary and secondary prevention. Despite the demonstrated efficacy of statins and ezetimibe on low-density lipoprotein (LDL) concentration and long-term CVD risk, a large number of patients do not achieve their therapeutic goals. The introduction of monoclonal antibodies against proprotein convertase subtilisin/kexin type 9 (PCSK9) protein was a milestone in the treatment of lipid disorders, as their administration leads to unprecedentedly low LDL cholesterol concentrations. Inclisiran represents an entirely new mechanism of PSCK9 protein inhibition in hepatocytes, targeting the messenger RNA for PCSK9. Its administration is necessary only every 3 to 6 months, which is an essential advantage over statin and monoclonal antibody therapy. The infrequent administration regimen can increase the number of patients who maintain their therapeutic goals, especially in patients struggling to comply with daily or biweekly pharmacotherapy. Preclinical studies and Phase I and Phase II clinical trials of inclisiran have demonstrated its tolerability and efficacy in promoting long-term reduction of both PCSK9 protein and LDL cholesterol. The efficacy and safety of inclisiran will continue to be assessed in ongoing and forthcoming trials on larger patient groups. If the results of these trials reflect previously published data, they will add further evidence that inclisiran might be a revolutionary new tool in the pharmacologic management of plasma lipids. This review summarizes the currently available literature data on inclisiran with respect to its mechanism of action, effectiveness, and safety as a lipid-lowering drug for CVD prevention.

在一级预防和二级预防中，已证明降低血浆中载脂蛋白B脂蛋白血浆浓度的药物可降低心血管疾病（CVD）的风险。尽管他汀类药物和依折麦布在低密度脂蛋白（LDL）浓度和长期CVD风险方面显示出疗效，但仍有大量患者无法达到治疗目的。抗原蛋白转化酶枯草杆菌蛋白酶/ kexin 9型（PCSK9）蛋白单克隆抗体的引入是治疗脂质疾病的一个里程碑，因为其给药可导致前所未有的低LDL胆固醇浓度。Inclisiran代表了一种针对PCSK9信使RNA的肝细胞中PSCK9蛋白抑制的全新机制。仅每3到6个月就需要对其进行管理，与他汀和单克隆抗体疗法相比，这是一个重要的优势。不频繁的给药方案可以增加维持治疗目标的患者数量，尤其是在每天或每两周一次药物治疗不力的患者中。inclisiran的临床前研究以及I期和II期临床试验表明，它具有促进PCSK9蛋白和LDL胆固醇长期降低的耐受性和功效。在持续和即将进行的针对更大患者群体的试验中，将继续评估inclisiran的疗效和安全性。如果这些试验的结果反映了以前发表的数据，那么它们将增加进一步的证据，表明inclisiran可能是血浆脂质药理学管理方面的革命性新工具。