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Published on: February 28, 2012
New oral anticoagulant drugs in cardiovascular disease
Ingo Ahrens1, Gregory Y H Lip, Karlheinz Peter
1Innere Medizin III, Kardiologie und Angiologie, Universitätsklinik, Hugstetter Strasse 55, Freiburg, Germany. ingo.ahrens@uniklinik-freiburg.de
Abstract:
Oral anticoagulation has been limited to vitamin K antagonists (VKAs) for over 60 years. VKAs are effective and recommended for the prevention of venous and arterial thromboembolism in cardiovascular disease, but their pharmacodynamics are difficult to predict and the highly variable interindividual and intraindividual response to treatment accounts for the need of continuous monitoring. This prompted the intensive exploration of numerous substances within the last decade in an attempt to meet the shortcomings of current oral anticoagulation with VKAs. The development and clinical investigation of two novel groups of oral anticoagulants targeting central factors of the coagulation system either factor Xa or thrombin (factor IIa) has now reached the daily clinical practice with the approval of the oral direct thrombin inhibitor dabigatran etexilate and the oral direct factor Xa inhibitor rivaroxaban. Ongoing clinical trials are investigating these substances and other novel oral anticoagulants with similar mechanisms of action in patients with atrial fibrillation and acute coronary syndromes. This review article discusses the clinical evaluation and pharmacological properties of novel oral anticoagulants in late and earlier stages of clinical development, thereby providing a critical analysis and an outlook on the future of oral anticoagulation in cardiovascular disease.
Insights
Novel oral anticoagulants offer an alternative to traditional vitamin K antagonists (VKAs) for preventing thromboembolism. These new drugs, targeting factor Xa or thrombin, aim to improve predictability and reduce monitoring needs in cardiovascular disease management.
Area of Science:
- Cardiology
- Pharmacology
- Hematology
Background:
- Oral anticoagulation has relied on vitamin K antagonists (VKAs) for over 60 years.
- VKAs require continuous monitoring due to unpredictable pharmacodynamics and variable patient response.
- Shortcomings of VKAs necessitate the development of alternative oral anticoagulants.
Purpose of the Study:
- To review the clinical evaluation and pharmacological properties of novel oral anticoagulants (NOACs).
- To critically analyze NOACs in late and earlier stages of clinical development.
- To provide an outlook on the future of oral anticoagulation in cardiovascular disease.
Main Methods:
- Review of clinical trials and pharmacological data for NOACs.
- Focus on direct thrombin inhibitors and direct factor Xa inhibitors.
- Analysis of NOACs in the context of cardiovascular disease, including atrial fibrillation and acute coronary syndromes.
Main Results:
- Novel oral anticoagulants targeting factor Xa or thrombin (factor IIa) are now in clinical practice.
- Dabigatran etexilate (direct thrombin inhibitor) and rivaroxaban (direct factor Xa inhibitor) have been approved.
- Ongoing trials investigate these and other NOACs for various cardiovascular conditions.
Conclusions:
- NOACs represent a significant advancement over VKAs, potentially offering improved predictability and reduced monitoring.
- These agents are increasingly integrated into the management of thromboembolic disorders in cardiovascular disease.
- The future of oral anticoagulation in cardiovascular disease is likely to involve a greater role for NOACs.
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