TY - JOUR
T1 - Apixaban
T2 - An oral direct factor-Xa inhibitor
AU - Jiménez, David
AU - Yusen, Roger D.
AU - Ramacciotti, Eduardo
N1 - Funding Information:
Editorial assistance was provided by Carol Cooper, PhD, of Caudex Medical, funded by Bristol-Myers Squibb and Pfizer Inc., and consisted solely of manuscript formatting; no contribution was made to intellectual content. All authors meet the criteria for authorship as per the guidelines of the International Committee of Medical Journal Editors. D.J. is the guarantor for this article, and takes responsibility for the integrity of the work as a whole. D.J. received compensation for advisory-board membership from Boehringer-Ingelheim, Bayer HealthCare,
Funding Information:
Bristol-Myers Squibb, Leo Pharma, and Rovi, and lecture fees from Sanofi-Aventis, Boehringer-Ingelheim, Bayer HealthCare, Leo Pharma, and Rovi. R.D.Y. has received grants from Pfizer Inc., Bristol-Myers Squibb, Bayer HealthCare Pharmaceuticals, Agen Biomedical Ltd., ParinGenix Inc., National Institutes of Health (NIH), and National Heart, Lung and Blood Institute (NHLBI) in the past 3 years. He has also acted as a consultant for Bayer HealthCare Pharmaceuticals, GlaxoSmithKline Ltd., and Sanofi-Aventis, and as a legal consultant for Merck & Co. Inc., Ortho Pharmaceuticals, and Organon. E.R. is an employee of Bristol-Myers Squibb.
PY - 2012/3
Y1 - 2012/3
N2 - Apixaban is a highly selective, reversible, direct factor Xa inhibitor that inhibits both free factor Xa and prothrombinase activity, and clot-bound factor Xa activity. A predictable pharmacokinetic profile, multiple pathways of elimination, an improved bleeding profile relative to warfarin with a lack of other significant adverse events, and no need for routine anticoagulation monitoring make apixaban appealing. Apixaban is currently approved for venous thromboembolism (VTE) prophylaxis in total hip replacement and total knee replacement in Europe, Brazil, Australia, and New Zealand, and has been pre-approved in Indonesia and the Philippines. Completed phase 3 trials suggest that apixaban has promise as an alternative to aspirin and warfarin for prevention of stroke and systemic embolism in patients with atrial fibrillation. Results of a large phase 3 trial were the first to show a survival benefit for this new class of oral anticoagulants in patients with atrial fibrillation. In patients with acute coronary syndrome, apixaban added to dual antiplatelet therapy with aspirin and clopidogrel resulted in unacceptably high rates of major bleeding. In medically ill patients, an extended course of thromboprophylaxis with apixaban was not superior to a shorter course with enoxaparin, and was associated with significantly more major bleeding events than enoxaparin. Ongoing phase 3 trials will provide data regarding the efficacy and safety of apixaban for treatment of acute deep vein thrombosis and pulmonary embolism.
AB - Apixaban is a highly selective, reversible, direct factor Xa inhibitor that inhibits both free factor Xa and prothrombinase activity, and clot-bound factor Xa activity. A predictable pharmacokinetic profile, multiple pathways of elimination, an improved bleeding profile relative to warfarin with a lack of other significant adverse events, and no need for routine anticoagulation monitoring make apixaban appealing. Apixaban is currently approved for venous thromboembolism (VTE) prophylaxis in total hip replacement and total knee replacement in Europe, Brazil, Australia, and New Zealand, and has been pre-approved in Indonesia and the Philippines. Completed phase 3 trials suggest that apixaban has promise as an alternative to aspirin and warfarin for prevention of stroke and systemic embolism in patients with atrial fibrillation. Results of a large phase 3 trial were the first to show a survival benefit for this new class of oral anticoagulants in patients with atrial fibrillation. In patients with acute coronary syndrome, apixaban added to dual antiplatelet therapy with aspirin and clopidogrel resulted in unacceptably high rates of major bleeding. In medically ill patients, an extended course of thromboprophylaxis with apixaban was not superior to a shorter course with enoxaparin, and was associated with significantly more major bleeding events than enoxaparin. Ongoing phase 3 trials will provide data regarding the efficacy and safety of apixaban for treatment of acute deep vein thrombosis and pulmonary embolism.
KW - Acute coronary syndrome
KW - Anticoagulants
KW - Apixaban
KW - Atrial fibrillation
KW - Deep vein thrombosis
KW - Prevention
KW - Treatment
KW - Venous thromboembolism
UR - http://www.scopus.com/inward/record.url?scp=84858709224&partnerID=8YFLogxK
U2 - 10.1007/s12325-012-0003-2
DO - 10.1007/s12325-012-0003-2
M3 - Review article
C2 - 22354465
AN - SCOPUS:84858709224
SN - 0741-238X
VL - 29
SP - 187
EP - 201
JO - Advances in Therapy
JF - Advances in Therapy
IS - 3
ER -