Apixaban - Metabolism, Pharmacologic Properties and Drug Interactions

Abstract

Background: Apixaban is an oral, potent, highly selective, reversible and direct inhibitor of activated coagulation factor X, that is the end point of the intrinsic and extrinsic coagulation pathway. Additionally, apixaban has the capacity to indirectly inhibit thrombin-induced platelet aggregation. This new oral anticoagulant represents an immediate-release form of peroral drug with quick dissolution, linear pharmacokinetics, good bioavailability and rapid onset and offset of action. No clinically relevant age- or sex-dependent difference in the apixaban pharmacokinetics and pharmacodynamics which would lead to the modification of the dose exists, apixaban may even be administered with or without food. Its elimination is mediated by metabolism, renal elimination of unmodified drug and excretion in the gastrointestinal tract.

Objective: The authors aim to provide a review of currently available literature about apixaban.

Method: The authors summed-up the data from the scientific journals related to thrombosis and hemostasis and searched the available databases.

Results and conclusion: Apixaban has many advantages including predictable pharmacokinetics and pharmacodynamics, low number of drug and food interactions, and relatively wide therapeutic window.

Keywords: Apixaban; anti-Xa activity; bleeding; drug interactions; elimination; metabolism; new oral anticoagulants; pharmacology.