Current and future prospects for anticoagulant therapy: inhibitors of factor Xa and factor IIa.
Indirect systemic and direct oral factor Xa and direct oral factor IIa inhibitors with improved pharmacologic profiles compared with heparins and vitamin K antagonists are currently in clinical development. This overview focuses on the indirect antithrombin dependent pentasaccharide derivatives of idraparinux and on the most advanced oral direct inhibitors to factor Xa (rivaroxaban and apixaban) and IIa (dabigatran). Specifically, the results of dose-finding studies for the prevention of venous thromboembolism after elective orthopedic surgery, the results of dose-finding studies for treatment of acute venous thromboembolism including prolonged prophylaxis of recurrent events, and the designs of ongoing clinical trials are reviewed.
Harenberg
Job
J
Clinical Pharmacology Mannheim, Vascular Pharmacotherapy, Faculty of Medicine, University of Heidelberg, Mannheim, Germany. job.harenberg@med.ma.uni-heidelberg.de
Wehling
Martin
M
D054058:Acute Coronary Syndrome / Q000188:drug therapy; D000284:Administration, Oral; D000925:Anticoagulants / Q000008:administration & dosage / Q000627:therapeutic use*; D001281:Atrial Fibrillation / Q000188:drug therapy; D001384:Azetidines / Q000627:therapeutic use; D001562:Benzimidazoles / Q000627:therapeutic use; D001596:Benzylamines / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D000069604:Dabigatran; D065427:Factor Xa Inhibitors; D005998:Glycine / Q000031:analogs & derivatives / Q000627:therapeutic use; D006801:Humans; D007263:Infusions, Parenteral; D009025:Morpholines / Q000627:therapeutic use; D009844:Oligosaccharides / Q000627:therapeutic use; D010879:Piperazines / Q000627:therapeutic use; D011516:Prothrombin / Q000037:antagonists & inhibitors*; D011720:Pyrazoles / Q000627:therapeutic use; D011725:Pyridines / Q000627:therapeutic use; D011728:Pyridones / Q000627:therapeutic use; D000069552:Rivaroxaban; D013876:Thiophenes / Q000627:therapeutic use; D013917:Thrombin / Q000037:antagonists & inhibitors; D013927:Thrombosis / Q000188:drug therapy / Q000517:prevention & control; D054556:Venous Thromboembolism / Q000188:drug therapy / Q000517:prevention & control
D000925:Anticoagulants; D001384:Azetidines; D001562:Benzimidazoles; D001596:Benzylamines; D065427:Factor Xa Inhibitors; C507963:LY517717; D009025:Morpholines; D009844:Oligosaccharides; D010879:Piperazines; D011720:Pyrazoles; D011725:Pyridines; D011728:Pyridones; D013876:Thiophenes; C522181:apixaban; C426686:ximelagatran; C479958:idraparinux; D011516:Prothrombin; C025337:Factor IIa; D000069552:Rivaroxaban; D013917:Thrombin; D000069604:Dabigatran; D005998:Glycine