From proprotein convertase subtilisin/kexin type 9 to its inhibition: state-of-the-art and clinical implications

被引：31

作者：

Navarese, Eliano P. ^{[1
,2
]}

Kolodziejczak, Michalina ^{[1
,3
]}

Dimitroulis, Dimitrios ^{[1
,2
]}

Wolff, Georg ^{[1
,2
]}

Busch, Hans L. ^{[1
,2
]}

Devito, Fiorella ^{[1
,4
]}

Sionis, Alessandro ^{[5
]}

Ciccone, Marco Matteo ^{[1
,4
]}

机构：

[1] MED Res Network, SIRIO, Dusseldorf, Germany

[2] Univ Dusseldorf, Div Cardiol Pulmonol & Vasc Med, Dept Internal Med, Moorenstr 5, D-40225 Dusseldorf, Germany

[3] Univ Nicolaus Copernicus, Coll Med Bydgoszcz, Torun, Poland

[4] Univ Bari, DETO, Bari, Italy

[5] Hosp Santa Creu & Sant Pau, Dept Cardiol, Intens Cardiac Care Unit, Barcelona, Spain

来源：

EUROPEAN HEART JOURNAL-CARDIOVASCULAR PHARMACOTHERAPY | 2016年 / 2卷 / 01期

关键词：

Proprotein convertase subtilisin; kexin type 9 (PCSK9); PCSK9; inhibitors; Clinical perspectives; PLACEBO-CONTROLLED TRIAL; CORONARY-HEART-DISEASE; EVOLOCUMAB AMG 145; HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA; PLASMA PCSK9 LEVELS; MONOCLONAL-ANTIBODY; LDL CHOLESTEROL; MYOCARDIAL-INFARCTION; CARDIOVASCULAR EVENTS; REDUCING LIPIDS;

D O I：

10.1093/ehjcvp/pvv045

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

Statins are recommended as first-line therapy for patients with hypercholesterolaemia. A sizable proportion of patients, however, does not reach therapeutic goals, is statin intolerant, or, despite optimal statin therapy, is at high risk of ischaemic events. Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays a major role in lipid metabolism and several comorbidities. Monoclonal antibodies targeting PCSK9 are a new lipid-lowering approach with the potential to improve clinical outcomes in patients with dyslipidaemia. In this review, we discuss current experimental and clinical evidence of the role of PCSK9 and its inhibition on lipid metabolism and several pathologic conditions with a focus on clinical outcomes. A state-of-the-art analysis of current clinical evidence and future directions on PCSK9 and its inhibition is provided.

引用

页码：44 / 53

页数：10

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