Dabigatran: an oral novel potent reversible nonpeptide inhibitor of thrombin.

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Eisert WG, Hauel N, Stangier J, Wienen W, Clemens A, van Ryn J

Dabigatran: an oral novel potent reversible nonpeptide inhibitor of thrombin.

Arterioscler Thromb Vasc Biol. 2010 Oct;30(10):1885-9. doi: 10.1161/ATVBAHA.110.203604. Epub 2010 Jul 29.

PubMed ID

20671233 [ View in PubMed

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Abstract

Dabigatran is a highly selective, reversible, and potent thrombin inhibitor and is orally available as the prodrug, dabigatran etexilate. It has shown antithrombotic efficacy in animal models of thrombosis, with a rapid onset of action and predictable pharmacodynamic response. Peak plasma concentrations of dabigatran occur 1 to 2 hours after ingestion of the prodrug. The terminal half-life of dabigatran is 12 to 14 hours in elderly volunteers. Dabigatran is not metabolized by cytochrome P450 isoenzymes and does not interact with food. Dabigatran has a low potential for drug-drug interactions and is predominantly renally excreted. Dabigatran etexilate as chronic therapy effectively prevents the recurrence of venous thromboembolism and cardioembolic stroke. For the first time, it has been demonstrated clinically that there may be an effective and safe alternative to warfarin.

DrugBank Data that Cites this Article

Drugs

Dabigatran etexilate

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Dabigatran etexilate	Prothrombin	Protein	Humans	Yes	Inhibitor	Details