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Cardiovascular diseases, including thromboembolic diseases associated with the western life style are major causes of morbidity and mortality in our society. The major components of hemostatic system are thrombocytes, the coagulation proteins and the fibrinolytic system. Therapies for thromboembolic diseases are based on different approaches depending on the site in the vascular system that is at risk when the disease occurs. Antithrombotic therapy has progressed enormously over the last two decades. Enormous attention from academic as well as pharma companies and biotech industry has resulted in novel agents for the prevention and treatment of thromboembolic diseases (Reopro, Clopidogrel, low molecular weight heparins, Exanta, Actilyse). As evidenced by the observation that many companies have projects in different stages of discovery and development in their pipeline, current therapy still leaves enough room for the development of novel antiplatelet, anticoagulant, and thrombolytic agents. Attention on the improvement of new agents is focused on but not restricted to the development of more efficient therapies but special focus in this area is also given to the ease of use, no need for therapy monitoring, oral availability, duration of action and the absence of side effects such as bleeding. Recent developments in drug discovery technology, such as combinatorial chemistry, high throughput screening, molecular modeling, pharmacogenomic guided screening, gene inactivation strategies, new targets as well as enhanced development processes will most probably contribute significantly to the medical therapy in the future. A contemporary overview of the approaches that might lead to novel products and the available literature are reviewed in this issue. Approaches for the development of antiplatelet agents, anticoagulant therapies and profibrinolytic treatments are addressed by the authors. Our special thanks go to the contributors of this issue.