Thrombotic events in cardiovascular disease are a huge burden to healthcare budgets. Anticoagulant use is recommended for thrombotic event prevention in many cardiovascular diseases, including stroke prevention in atrial fibrillation, treatment and secondary prevention of acute coronary syndrome. Current parenteral anticoagulants include unfractionated heparin, low-molecular-weight heparins (LMWHs) and fondaparinux. Patients with acute coronary syndrome usually receive unfractionated heparin or a LMWH on hospital admission, both exhibit similar efficacy in reducing mortality and myocardial infarction rates; however, LMWHs may have a better safety profile and do not require routine coagulation monitoring. In acute coronary syndrome, fondaparinux use results in significantly lower mortality compared with LMWHs or unfractionated heparin. However, parenteral drugs are inconvenient for long-term outpatient use. Vitamin K antagonists are currently the only oral anticoagulants available for long-term use, but multiple drawbacks hinder their use. A large unmet need exists for new convenient and well-tolerated oral anticoagulants that do not require routine monitoring.