Dabigatran: an oral novel potent reversible nonpeptide inhibitor of thrombin.
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.
Eisert
Wolfgang G
WG
Clinical Development and Medical Affairs, Boehringer Ingelheim GmbH, 172 Binger St, Ingelheim 55216, Germany. eisert@ing.boehringer-ingelheim.com
Hauel
Norbert
N
Stangier
Joachim
J
Wienen
Wolfgang
W
Clemens
Andreas
A
van Ryn
Joanne
J
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*
D000925:Anticoagulants; D001562:Benzimidazoles; D011355:Prodrugs; D011725:Pyridines; D013917:Thrombin; D000069604:Dabigatran