Proprotein convertase subtilisin kexin 9 inhibitors: Current status and future directions

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PCSK9 (Proprotein convertase subtilisin/kexin type 9) inhibitors: past, present, and the future.

Reduction in low-density lipoprotein cholesterol (LDL-C), mainly with statins, has decreased the risk of cardiovascular events over the last few decades. However, there are several patient populations that warrant further decrease in LDL-C by additional cholesterol-lowering therapy other than statins. Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors are a new class of drugs that...

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Increased Risk of Adverse Neurocognitive Outcomes With Proprotein Convertase Subtilisin-Kexin Type 9 Inhibitors.

BACKGROUND There is encouraging evidence of the efficacy of proprotein convertase subtilisin-kexin type 9 (PCSK9) inhibitors; however, their long-term safety remains unclear. We performed a meta-analysis of studies to evaluate the long-term safety of PCSK9 inhibitors. METHODS AND RESULTS Our search strategy yielded 11 studies (9 smaller early-phase and 2 larger outcome trials). The outcomes a...

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Identification of Potential Inhibitors for Lowering Cholesterol Level by Inhibiting Proprotein Convertase Subtilisin Kexin 9

Objective: Proprotein convertase subtilisin kexin 9 (PCSK9) has medical significance in lowering cholesterol levels. Inhibitors target and inactivate PCSK9 in the liver. Knocking out PCSK9 reduces the amount of harmful low-density lipoprotein cholesterol (LDL-C) circulating in the bloodstream. There are two known inhibitors for treating the cardiovascular disease “Arilocumab” and “Evalocumab.” ...

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Statins, plasma proprotein convertase subtilisin/kexin type 9 concentrations, and LDL lowering.

The discovery in 2003 that variants in the PCSK9 (proprotein convertase subtilisin/kexin type 9) gene cause autosomal dominant hypercholesterolemia revealed a new aspect of LDL cholesterol (LDL-C) metabolism (1). PCSK9, a protein of 692 amino acid residues produced at high concentrations in the liver, kidney, and intestine, has profound effects on LDL-C concentrations (2). Both gain-of-function...

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Rosuvastatin, proprotein convertase subtilisin/kexin type 9 concentrations, and LDL cholesterol response: the JUPITER trial.

BACKGROUND Although statin therapy is known to increase concentrations of PCSK9, whether this effect is related to the magnitude of LDL reduction is uncertain. This study was undertaken to understand the extent of this effect and examine the relationship between PCSK9 and LDL cholesterol (LDL-C) reduction. METHODS We measured plasma PCSK9 concentrations by ELISA at baseline and at 1 year in 5...

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ژورنال

عنوان ژورنال: Journal of Clinical and Preventive Cardiology

سال: 2017

ISSN: 2250-3528

DOI: 10.4103/2250-3528.196649