Advances in the field of proprotein convertase subtilisin kexin type 9 inhibitors.

Abstract:

PURPOSE OF REVIEW:Proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitors are promising therapies that inhibit the degradation of low-density lipoprotein (LDL) receptors in the hepatocyte and thus increase LDL cholesterol (LDL-C) uptake from the blood. This review summarizes main findings in the field of PCSK9 inhibitors, from basic mechanism to clinical studies, and aims to provide a contemporary and practical overview of the clinical implication and future directions with PCSK9 inhibitors. RECENT FINDINGS:Monoclonal antibodies that inhibit PCSK9 reduce LDL-C levels by 40-70% across a wide range of patients with various LDL-C levels, and with different lipid-lowering regimens. These agents significantly reduce apolipoprotein B and lipoprotein (a), may have a potential role in plaque stabilization in acute coronary syndromes, and are safe and tolerable, even among statin-intolerant patients. Preliminary data with evolocumab and alirocumab demonstrate the potential reduction of cardiovascular (CV) events. These PCSK9 inhibitors were recently approved for clinical use, and recommended in the 2016 American College of Cardiology expert consensus document for nonstatin therapy for LDL-C lowering. SUMMARY:PCSK9 inhibitors are novel promising therapies to reduce LDL-C. Ongoing phase 3 clinical trials with more than 70 000 high-risk patients will examine their safety and efficacy in reducing cardiovascular disease.

journal_name

Curr Opin Cardiol

authors

Eisen A,Giugliano RP

doi

10.1097/HCO.0000000000000332

subject

Has Abstract

pub_date

2016-11-01 00:00:00

pages

644-653

issue

6

eissn

0268-4705

issn

1531-7080

journal_volume

31

pub_type

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