Abstract
Atrial fibrillation is a major risk factor for first and recurrent ischaemic stroke, and anticoagulation, mainly by use of coumarin medications, is an effective strategy for reducing ischaemic stroke occurrence in these patients. However, the coumarin medications have disadvantages. Over the past decade, important strides have been made towards developing improved anticoagulant medications. This review discusses these new developments and what they mean for the future of primary and secondary ischaemic stroke prevention in patients with atrial fibrillation. Relevant papers were identified with electronic searches of the Medline and EMBASE databases. Ongoing trials were checked using the Trials Results Centre website. The direct thrombin inhibitors, and the factor Xa inhibitors are the two major new anticoagulant drug classes under development at present. In phase III trials, dabigatran and rivaroxaban demonstrated at least as good performance as warfarin at reducing the rate of ischaemic stroke, systemic embolus, and haemorrhagic ischaemic stroke, whilst maintaining a comparable or lower rate of major bleeding events. Drug level monitoring was not required due to stable pharmacodynamics. AZD0837, apixaban, YM-150, edoxaban and betrixaban all showed promising results in phase II trials, as did S35972 in animal, in vitro and ex vivo models. The future of these new anticoagulants looks encouraging, although there are still some significant challenges to overcome. We need to consider the accumulation of long-term safety and efficacy data, and the development of effective means of reversal of anticoagulation for the direct thrombin inhibitors and factor Xa inhibitors.
Keywords: Anticoagulant, antithrombotic, factor Xa inhibitors, thrombin inhibitors, atrial fibrillation, ischaemic stroke, primary and secondary stroke prevention.
CNS & Neurological Disorders - Drug Targets
Title:New Thrombin and Factor Xa Inhibitors for Primary and Secondary Prevention of Ischaemic Stroke
Volume: 12 Issue: 2
Author(s): Lisa Winstanley and Ruoling Chen
Affiliation:
Keywords: Anticoagulant, antithrombotic, factor Xa inhibitors, thrombin inhibitors, atrial fibrillation, ischaemic stroke, primary and secondary stroke prevention.
Abstract: Atrial fibrillation is a major risk factor for first and recurrent ischaemic stroke, and anticoagulation, mainly by use of coumarin medications, is an effective strategy for reducing ischaemic stroke occurrence in these patients. However, the coumarin medications have disadvantages. Over the past decade, important strides have been made towards developing improved anticoagulant medications. This review discusses these new developments and what they mean for the future of primary and secondary ischaemic stroke prevention in patients with atrial fibrillation. Relevant papers were identified with electronic searches of the Medline and EMBASE databases. Ongoing trials were checked using the Trials Results Centre website. The direct thrombin inhibitors, and the factor Xa inhibitors are the two major new anticoagulant drug classes under development at present. In phase III trials, dabigatran and rivaroxaban demonstrated at least as good performance as warfarin at reducing the rate of ischaemic stroke, systemic embolus, and haemorrhagic ischaemic stroke, whilst maintaining a comparable or lower rate of major bleeding events. Drug level monitoring was not required due to stable pharmacodynamics. AZD0837, apixaban, YM-150, edoxaban and betrixaban all showed promising results in phase II trials, as did S35972 in animal, in vitro and ex vivo models. The future of these new anticoagulants looks encouraging, although there are still some significant challenges to overcome. We need to consider the accumulation of long-term safety and efficacy data, and the development of effective means of reversal of anticoagulation for the direct thrombin inhibitors and factor Xa inhibitors.
Export Options
About this article
Cite this article as:
Winstanley Lisa and Chen Ruoling, New Thrombin and Factor Xa Inhibitors for Primary and Secondary Prevention of Ischaemic Stroke, CNS & Neurological Disorders - Drug Targets 2013; 12 (2) . https://dx.doi.org/10.2174/18715273112119990051
DOI https://dx.doi.org/10.2174/18715273112119990051 |
Print ISSN 1871-5273 |
Publisher Name Bentham Science Publisher |
Online ISSN 1996-3181 |
Call for Papers in Thematic Issues
Diagnosis and treatment of central nervous system infectious diseases
Infectious diseases of the central nervous system (CNS) can be divided into bacterial, tuberculous, viral, fungal, parasitic infections, etc. Early etiological treatment is often the most crucial means to reduce the mortality rate of patients with central nervous system infections, reduce complications and sequelae, and improve prognosis. The initial clinical ...read more
Techniques of Drug Repurposing: Delivering a new life to Herbs & Drugs
Of late, with the adaptation of innovative approaches and integration of advancements made towards medical sciences as well as the availability of a wide range of tools; several therapeutic challenges are being translated into viable clinical solutions, with a high degree of efficacy, safety, and selectivity. With a better understanding ...read more
Trends and perspectives in the rational management of CNS disorders
Central nervous system (CNS) diseases enforce a significant global health burden, driving ongoing efforts to improve our understanding and effectiveness of therapy. This issue investigates current advances in the discipline, focusing on the understanding as well as therapeutic handling of various CNS diseases. The issue covers a variety of diseases, ...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
-
Imaging Epigenetics in Alzheimer’s Disease
Current Pharmaceutical Design Pharmacological Inhibition of Protein Tyrosine Phosphatase 1B: A Promising Strategy for the Treatment of Obesity and Type 2 Diabetes Mellitus
Current Medicinal Chemistry A Point of View: The Need to Identify an Antigen in Psyconeuroimmunological Disorders
Current Pharmaceutical Design Calix[n]arenes as Goldmines for the Development of Chemical Entities of Pharmaceutical Interest
Current Pharmaceutical Design N-Methyl D-Aspartate (NMDA) Receptor Antagonists and Memantine Treatment for Alzheimer’s Disease, Vascular Dementia and Parkinson’s Disease
Current Alzheimer Research Cholesterol, Alzheimers Disease, Prion Disorders: A menage a trois?
Current Drug Targets Modulatory Effects of pH, Cu+2 and Sheet Breakers on Aggregation of Amyloid Peptides
Protein & Peptide Letters Quinoline Derivatives: Candidate Drugs for a Class B G-Protein Coupled Receptor, the Calcitonin Gene-Related Peptide Receptor, a Cause of Migraines
CNS & Neurological Disorders - Drug Targets Rationally Designed Multi-Targeted Agents Against Neurodegenerative Diseases
Current Medicinal Chemistry Therapeutic Approaches Targeting Pathological Tau Aggregates
Current Pharmaceutical Design Nanoparticle-Encapsulated Bryostatin-1 Activates α-Secretase and PKC Isoforms In vitro and Facilitates Acquisition and Retention of Spatial Learning in an Alzheimer's Disease Mouse Model
Current Alzheimer Research Development and Potential Utility of Dual and Triple NK Receptor Antagonists
Current Topics in Medicinal Chemistry miR-132 Down-regulates Methyl CpG Binding Protein 2 (MeCP2) During Cognitive Dysfunction Following Chronic Cerebral Hypoperfusion
Current Neurovascular Research Effect of Polyherbal Drug Majun Falasfa on the Transgenic Drosophila Model of Parkinson’s Disease
Current Traditional Medicine Erratum
Current Alzheimer Research Phosphorylation-Dephosphorylation Imbalance of Cytoskeletal Associated Proteins in Neurodegenerative Diseases
Recent Patents on CNS Drug Discovery (Discontinued) The Clinical and Biological Relationship between Type II Diabetes Mellitus and Alzheimers Disease
Current Alzheimer Research Effects of SORL1 Gene on Alzheimer's Disease. Focus on Gender, Neuropsychiatric Symptoms and Pro-Inflammatory Cytokines
Current Alzheimer Research Type 2 Diabetes Mellitus and the Elderly: An Update on Drugs Used to Treat Glycaemia
Current Vascular Pharmacology Targeting Parkinson’s - Tyrosine Hydroxylase and Oxidative Stress as Points of Interventions
CNS & Neurological Disorders - Drug Targets