Dabigatran etexilate is a double prodrug that undergoes in vivo hydrolytic cleavage to produce dabigatran , a potent thrombin inhibitor (Ki = 4.5 nM). Dabigatran also inhibits trypsin (Ki = 50.3 nM), but only weakly inhibits other serine proteases. The prodrug dabigatran etexilate shows antithrombotic efficacy in animal models of thrombosis, with a rapid onset of action. It is not metabolized by cytochrome P450 isozymes and has a low potential for drug-drug interactions.
