The role of PCSK9 in intestinal lipoprotein metabolism: Synergism of statin and ezetimibe

Sergio Fazio

doi:10.1016/S1567-5688(15)50006-8

The role of PCSK9 in intestinal lipoprotein metabolism: Synergism of statin and ezetimibe

Sergio Fazio

Research output: Contribution to journal › Article

6 Scopus citations

Abstract

Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays a major role in the regulation of lipoprotein metabolism, mostly through control of low-density lipoprotein receptor degradation. Depletion of cellular cholesterol causes a compensatory increase in plasma PCSK9 levels, which can diminish the cholesterol-lowering power of statins and may lead to the overproduction of intestinal lipoproteins, mainly thorough the up regulation of microsomal triglyceride transfer protein and the Niemann-Pick C1-like 1 protein, the target of ezetimibe. Thus, ezetimibe therapy may counter this unwanted effect of statins, providing an additional theoretical rationale for combining the effect of ezetimibe on intestinal cholesterol absorption and that of statins on cholesterol synthesis.

Original language	English (US)
Pages (from-to)	23-26
Number of pages	4
Journal	Atherosclerosis Supplements
Volume	17
DOIs	https://doi.org/10.1016/S1567-5688(15)50006-8
State	Published - Feb 1 2015

Keywords

Ezetimibe
LDL receptor

ASJC Scopus subject areas

Internal Medicine
Cardiology and Cardiovascular Medicine

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10.1016/S1567-5688(15)50006-8

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Fazio, S. (2015). The role of PCSK9 in intestinal lipoprotein metabolism: Synergism of statin and ezetimibe. Atherosclerosis Supplements, 17, 23-26. https://doi.org/10.1016/S1567-5688(15)50006-8

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abstract = "Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays a major role in the regulation of lipoprotein metabolism, mostly through control of low-density lipoprotein receptor degradation. Depletion of cellular cholesterol causes a compensatory increase in plasma PCSK9 levels, which can diminish the cholesterol-lowering power of statins and may lead to the overproduction of intestinal lipoproteins, mainly thorough the up regulation of microsomal triglyceride transfer protein and the Niemann-Pick C1-like 1 protein, the target of ezetimibe. Thus, ezetimibe therapy may counter this unwanted effect of statins, providing an additional theoretical rationale for combining the effect of ezetimibe on intestinal cholesterol absorption and that of statins on cholesterol synthesis.",

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