title: Dabigatran: an oral novel potent reversible nonpeptide inhibitor of thrombin.
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.
authors.affiliation: Clinical Development and Medical Affairs, Boehringer Ingelheim GmbH, 172 Binger St, Ingelheim 55216, Germany. eisert@ing.boehringer-ingelheim.com
authors.forename: Wolfgang G
authors.initials: WG
authors.lastname: Eisert
authors.forename: Norbert
authors.initials: N
authors.lastname: Hauel
authors.forename: Joachim
authors.initials: J
authors.lastname: Stangier
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Wienen
authors.forename: Andreas
authors.initials: A
authors.lastname: Clemens
authors.forename: Joanne
authors.initials: J
authors.lastname: van Ryn
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000925:Anticoagulants / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001562:Benzimidazoles / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D000069604:Dabigatran; D015195:Drug Design; D006801:Humans; D066298:In Vitro Techniques; D011355:Prodrugs / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D011725:Pyridines / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D013917:Thrombin / Q000037:antagonists & inhibitors*
chemical_list: D000925:Anticoagulants; D001562:Benzimidazoles; D011355:Prodrugs; D011725:Pyridines; D013917:Thrombin; D000069604:Dabigatran