The anticoagulant drugs have an essential role in the prevention and treatment of thromboembolic diseases. The currently available anticoagulants have several limitations, including a narrow therapeutic window, the risk of bleeding complications and, for some drugs, the need for laboratory monitoring and parenteral administration. These limitations make the case for the development of new anticoagulants. An ideal anticoagulant should be effective, safe, simple to use, and widely applicable. The new anticoagulants currently under investigation are obtained by molecular technology that makes it possible to target their effect toward a selected step of the coagulation cascade. Based on their target, new anticoagulants can be classified into three groups: inhibitors of activation of coagulation, inhibitors of propagation of coagulation, and inhibitors of thrombin formation. Several new anticoagulants currently are in different phases of development. Some of them have been approved for clinical use, others are in advanced phase of clinical development, and some are still in the initial phase of investigation.