Rivaroxaban, an oral direct factor Xa inhibitor.
Rivaroxaban is a small molecule, direct Factor Xa inhibitor and may be a potentially attractive alternative to vitamin K antagonists. Rivaroxaban is being investigated for the prevention and treatment of venous and arterial thrombosis. A broad search of Medline, clinicaltrials.gov and the annual proceedings of the American Society of Hematology and the International Society on Thrombosis and Hemostasis was conducted. This review addresses the findings of this systematic search, including the need for new oral anticoagulants, the development and pharmacology of rivaroxaban, and the results of completed as well as ongoing trials with rivaroxaban. At present, the safety and efficacy of rivaroxaban for the prophylaxis and treatment of venous thromboembolism has been evaluated in Phase II and Phase III trials involving over 24,000 patients. Additionally, rivaroxaban is being evaluated for the treatment of pulmonary embolism, secondary prevention after acute coronary syndromes and the prevention of stroke and non-central nervous system embolism in patients with non-valvular atrial fibrillation. The drug may have its greatest impact in providing a much-needed and attractive alternative to warfarin. Further data (especially large Phase III trials) are required.
Piccini
Jonathan P
JP
Duke University Medical Center, Duke Clinical Research Institute, 2400 Pratt Street, #7581, Durham, NC 27705, USA. jonathan.piccini@duke.edu
Patel
Manesh R
MR
Mahaffey
Kenneth W
KW
Fox
Keith A A
KA
Califf
Robert M
RM
D054058:Acute Coronary Syndrome / Q000150:complications / Q000188:drug therapy; D000284:Administration, Oral; D000368:Aged; D000369:Aged, 80 and over; D000818:Animals; D000925:Anticoagulants / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D001281:Atrial Fibrillation / Q000150:complications / Q000188:drug therapy; D001665:Binding Sites / Q000187:drug effects; D002986:Clinical Trials as Topic / Q000706:statistics & numerical data; D015897:Comorbidity; D004353:Drug Evaluation, Preclinical; D015951:Factor Xa / Q000737:chemistry; D065427:Factor Xa Inhibitors; D005343:Fibrinolytic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D006470:Hemorrhage / Q000139:chemically induced; D006801:Humans; D008297:Male; D008875:Middle Aged; D009025:Morpholines / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D011183:Postoperative Complications / Q000517:prevention & control; D051381:Rats; D000069552:Rivaroxaban; D020521:Stroke / Q000453:epidemiology / Q000209:etiology / Q000517:prevention & control; D013876:Thiophenes / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D013927:Thrombosis / Q000188:drug therapy / Q000209:etiology / Q000517:prevention & control*; D014859:Warfarin / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use
D000925:Anticoagulants; D065427:Factor Xa Inhibitors; D005343:Fibrinolytic Agents; D009025:Morpholines; D013876:Thiophenes; D014859:Warfarin; D000069552:Rivaroxaban; D015951:Factor Xa