Abstract
Statins are the most widely prescribed drugs to reduce serum low density lipoprotein cholesterol (LDL-C) by inhibiting 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase. LDL-C reduction is associated with a decreased risk of atherosclerotic cardiovascular disease (ASCVD), including cardiovascular disease (CVD) and stroke. Statins reduce LDL-C by 30 to 40%, and the combination with other lipid-lowering agents such as ezetimibe leads to a further reduction by 20 to 25%. However, even the combination of these two agents might not be sufficient in high risk patients to require aggressive LDL-C reduction. Therefore, starting from observations on individuals with loss-of-function in proprotein convertase subtilisin/kexin type 9 (PCSK9), which was associated with lower LDL-C levels and CVD rates, monoclonal antibodies (mAbs) against PCSK9 were developed. To date, two mAbs, alirocumab and evolocumab, have received approval by the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA). In the present review we give an overview about pathophysiological and clinical aspects as well as evidence for these drugs with respect to cerebrovascular events.
Keywords: Alirocumab, evolocumab, LDL-cholesterol, PCSK9, proprotein convertase subtilisin/kexin type 9, stroke.
Cardiovascular & Hematological Agents in Medicinal Chemistry
Title:Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9): Impact of PCSK9 on Major Adverse Cardiac and Cerebrovascular Events
Volume: 14 Issue: 2
Author(s): Muharrem Akin, Thomas Skripuletz, L. Christian Napp, Dominik Berliner, Ibrahim Akin, Arash Haghikia, Elvan Akin and Johann Bauersachs
Affiliation:
Keywords: Alirocumab, evolocumab, LDL-cholesterol, PCSK9, proprotein convertase subtilisin/kexin type 9, stroke.
Abstract: Statins are the most widely prescribed drugs to reduce serum low density lipoprotein cholesterol (LDL-C) by inhibiting 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase. LDL-C reduction is associated with a decreased risk of atherosclerotic cardiovascular disease (ASCVD), including cardiovascular disease (CVD) and stroke. Statins reduce LDL-C by 30 to 40%, and the combination with other lipid-lowering agents such as ezetimibe leads to a further reduction by 20 to 25%. However, even the combination of these two agents might not be sufficient in high risk patients to require aggressive LDL-C reduction. Therefore, starting from observations on individuals with loss-of-function in proprotein convertase subtilisin/kexin type 9 (PCSK9), which was associated with lower LDL-C levels and CVD rates, monoclonal antibodies (mAbs) against PCSK9 were developed. To date, two mAbs, alirocumab and evolocumab, have received approval by the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA). In the present review we give an overview about pathophysiological and clinical aspects as well as evidence for these drugs with respect to cerebrovascular events.
Export Options
About this article
Cite this article as:
Akin Muharrem, Skripuletz Thomas, Napp Christian L., Berliner Dominik, Akin Ibrahim, Haghikia Arash, Akin Elvan and Bauersachs Johann, Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9): Impact of PCSK9 on Major Adverse Cardiac and Cerebrovascular Events, Cardiovascular & Hematological Agents in Medicinal Chemistry 2016; 14 (2) . https://dx.doi.org/10.2174/1871525714666160727113740
DOI https://dx.doi.org/10.2174/1871525714666160727113740 |
Print ISSN 1871-5257 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6182 |
Call for Papers in Thematic Issues
Medicinal Plants with Beneficial Properties on Diabetes and Hypertension
Diabetes and hypertension are real scourges of the 21st century. It is imperative to act in order to find innovative solutions to this problem. Taking medications such as hypoglycemic and antihypertensive drugs may aggravate certain underlying comorbidities, such as chronic kidney disease and cardiovascular disease. This significant drawback therefore requires ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Reversal in Cognition Impairments, Cholinergic Dysfunction, and Cerebral Oxidative Stress Through the Modulation of Ryanodine Receptors (RyRs) and Cysteinyl Leukotriene-1 (CysLT1) Receptors
Current Neurovascular Research Prognosis and Treatment of Ventricular Arrhythmias Following Myocardial Infarction
Current Cardiology Reviews Recent Applications of Polyacrylamide as Biomaterials
Recent Patents on Materials Science Molecules to Selectively Target Receptors for Treatment of Pain and Neurogenic Inflammation
Recent Patents on Inflammation & Allergy Drug Discovery Disrupted Structural Brain Network in AD and aMCI: A Finding of Long Fiber Degeneration
Current Alzheimer Research LncRNAs a New Target for Post-Stroke Recovery
Current Pharmaceutical Design CETP Pharmacological Manipulation Transforming Human into Mouse: Is this Still a Viable Hypothesis?
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) The Role of Disproportionality Analysis of Pharmacovigilance Databases in Safety Regulatory Actions: a Systematic Review
Current Drug Safety Recent Advances in the Medicinal Chemistry of Sodium Channel Blockers and their Therapeutic Potential
Current Topics in Medicinal Chemistry Proteome Adjustments Post Gradual Hypoxic Stress in Barilius bendelisis: Insights into Adaptive Strategies of a Hill Stream Cyprinid
Current Proteomics Resveratrol Augments Doxorubicin and Cisplatin Chemotherapy: A Novel Therapeutic Strategy
Current Molecular Pharmacology Prevalence of Pre-Existing Risk Factors for Adverse Events Associated with Atypical Antipsychotics Among Commercially Insured and Medicaid Insured Patients Newly Initiating Atypical Antipsychotics
Current Drug Safety Recent Developments in Temperature Responsive Shape Memory Polymers
Mini-Reviews in Organic Chemistry Design and Development of Solid Dispersion of Valsartan by a Lyophilization Technique: A 3<sup>2</sup> Factorial Design Approach
Micro and Nanosystems The Pathophysiology of Sleep Apnoea: What We have Learned from Animal Models of Chronic Intermittent Hypoxia
Current Respiratory Medicine Reviews Modulators of Voltage-Dependent Calcium Channels for the Treatment of Nervous System Diseases
Recent Patents on CNS Drug Discovery (Discontinued) Hydroxyimine NO-Donors; FK409 and Derivatives
Current Topics in Medicinal Chemistry The Role of αA-Crystallin in Experimental Autoimmune Uveitis
Current Molecular Medicine Role of the Decreased Nitric Oxide Bioavailability in the Vascular Complications of Diabetes Mellitus
Current Pharmaceutical Biotechnology The Role of Antithrombotic Therapy in Heart Failure
Current Pharmaceutical Design