[Lipid control in high-risk patients: focus on PCSK9 inhibitors].

Abstract

Low-density lipoprotein (LDL)-cholesterol levels are strictly related to the risk of major cardiovascular events. Statins have been demonstrated to significantly reduce LDL-cholesterol levels, contributing to cardiovascular risk reduction especially in high-risk patients. However, low adherence to statins, due to adverse effects, is often observed and many patients in secondary prevention exhibit LDL-cholesterol levels >70 mg/dl. As a consequence, there is the need for new therapeutic approaches with different mechanisms of action to reach recommended lipid targets in high-risk patients. One potential approach is to inhibit PCSK9, a serum protein with an active role in controlling the expression of LDL receptors, by reducing their recycling and targeting it for lysosomal destruction. Monoclonal antibodies against PCSK9, in particular alirocumab and evolocumab, have been shown to reduce LDL substantially, either with or without concomitant statin therapy with good tolerability. Ongoing trials will further define the efficacy of these drugs as an emerging approach to the treatment of hypercholesterolemia in primary and secondary prevention of high-risk patients.

• Authors: Pasquale Perrone Filardi, Stefania Paolillo, Bruno Trimarco
• Journal: Giornale italiano di cardiologia (2006) (G Ital Cardiol (Rome)) Vol. 16 Issue 1 Pg. 44-51 (Jan 2015) ISSN: 1827-6806 [Print] Italy
• Vernacular Title: Controllo lipidico in pazienti ad elevato rischio cardiovascolare: focus sull'inibizione di PCSK9.
• PMID: 25689751 (Publication Type: Journal Article, Review)

Chemical References

• Antibodies, Monoclonal
• Antibodies, Monoclonal, Humanized
• Anticholesteremic Agents
• Cholesterol, LDL
• Hydroxymethylglutaryl-CoA Reductase Inhibitors
• Receptors, LDL
• PCSK9 protein, human
• Proprotein Convertase 9
• Proprotein Convertases
• Serine Endopeptidases
• evolocumab
• alirocumab

Topics

• Antibodies, Monoclonal (adverse effects, pharmacology, therapeutic use)
• Antibodies, Monoclonal, Humanized
• Anticholesteremic Agents (adverse effects, pharmacology, therapeutic use)
• Cardiovascular Diseases (etiology, prevention & control)
• Cholesterol, LDL (blood)
• Humans
• Hydroxymethylglutaryl-CoA Reductase Inhibitors (administration & dosage, adverse effects, therapeutic use)
• Hypercholesterolemia (complications, drug therapy)
• Proprotein Convertase 9
• Proprotein Convertases (antagonists & inhibitors, metabolism)
• Receptors, LDL (metabolism)
• Risk Factors
• Serine Endopeptidases (metabolism)