Pharmacodynamics, pharmacokinetics and clinical efficacy of apixaban in the treatment of thrombosis

ABSTRACT

Introduction: Venous thromboembolism (VTE) is a common disorder. Heparin and vitamin K antagonists have been the standard treatment for VTE for over 50 years. The development of apixaban and other direct oral anticoagulants has greatly increased the range of anticoagulants available for the treatment of VTE.

Area covered: Studies on the chemistry, pharmacodynamics and pharmacokinetics of apixaban are reviewed. Its clinical efficacy and safety are discussed, with an emphasis on randomized controlled Phase III clinical trials on treatment of thrombosis.

Expert opinion: Apixaban is a safe and effective anticoagulant for VTE treatment. It has several attractive features: its oral activity, rapid action, limited drug- interaction profile and limited need for laboratory monitoring. An antidote may become available in the near future. Further studies of certain patient populations such as patients with cancers, elderly (aged 75 years and older) and those with severe renal and liver disease, are required as these patients have not yet been studied in sufficient numbers. As clinical trials included only selected patients, data from these studies may not reflect the ‘real-life’ patients in clinical practice. There is therefore an unmet need for large post-registration studies of unselected ‘real-life’ patients, such as registry studies, to validate the clinical trial findings.

KEYWORDS:

• Anti-factor Xa
• apixaban
• oral anticoagulant
• venous thrombo-embolism

Declaration of interest

BH Chong was a site study investigator/collaborator of the Amplify and Amplify-Ext studies sponsored by Pfizer and Bristol-Meyers Squibb, Hokusai-VTE study (edoxaban) sponsored by Daiichi-Sankyo and Einstein DVT and Einstein PE studies sponsored by Bayer Healthcare (rivaroxaban). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.