Direct thrombin inhibitors.
Heparins and vitamin K antagonists have been the primary agents used for anticoagulation in certain cardiovascular and thromboembolic diseases for over 50 years. However, they can be difficult to administer and are fraught with limitations. In response to the need for new anticoagulants, direct thrombin inhibitors (DTIs) have been developed and investigated for their utility in prophylaxis and treatment of venous thromboembolism (VTE), heparin-induced thrombocytopenia (HIT), acute coronary syndromes (ACS), secondary prevention of coronary events after ACS, and nonvalvular atrial fibrillation. Currently, four parenteral direct inhibitors of thrombin activity are FDA-approved in North America: lepirudin, desirudin, bivalirudin and argatroban. Of the new oral DTIs, dabigatran etexilate is the most studied and promising of these agents. This review discusses the clinical indications and efficacy of these direct thrombin inhibitors as well as future directions in anticoagulant therapy.
Department of Medicine, Memorial Sloan-Kettering Cancer Center, New York, USA. leec@mskcc.org
Catherine J
CJ
Lee
Jack E
JE
Ansell
D000925:Anticoagulants / Q000494:pharmacology; D000991:Antithrombins / Q000494:pharmacology*; D001120:Arginine / Q000031:analogs & derivatives; D001562:Benzimidazoles / Q000627:therapeutic use; D000069604:Dabigatran; D006629:Hirudins / Q000494:pharmacology; D006801:Humans; D010446:Peptide Fragments / Q000494:pharmacology; D010875:Pipecolic Acids / Q000627:therapeutic use; D011725:Pyridines / Q000627:therapeutic use; D011994:Recombinant Proteins / Q000494:pharmacology; D013449:Sulfonamides; D013917:Thrombin / Q000037:antagonists & inhibitors / Q000627:therapeutic use; D054556:Venous Thromboembolism / Q000517:prevention & control
D000925:Anticoagulants; D000991:Antithrombins; D001562:Benzimidazoles; D006629:Hirudins; D010446:Peptide Fragments; D010875:Pipecolic Acids; D011725:Pyridines; D011994:Recombinant Proteins; D013449:Sulfonamides; D001120:Arginine; D013917:Thrombin; D000069604:Dabigatran; C031942:argatroban; C074619:bivalirudin
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