Oral IIa inhibitors.

Direct oral factor IIa inhibitors represent a new class of anticoagulants for the prevention and treatment of venous and selected arterial thomboembolisms. Dabigatran etexilate is the most studied and promising of the oral direct thrombin inhibitors. Preclinical and early-phase clinical studies show it to have a predictable and reliable pharmacokinetic and pharmacodynamic profile, whereas advanced phase 3 trials prove it to be noninferior to traditional anticoagulants in selective conditions for the prevention and treatment of venous and arterial thromboembolism. Other advantages of this drug, including a lack of interaction with cytochrome P450 enzymes or with food and drugs, rapid onset of action, good safety profile, lack of need for routine monitoring, broad therapeutic window, and fixed-dose administration, make this a competitive oral anticoagulant. Copyright 2010 Elsevier Inc. All rights reserved.