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Rivaroxaban was patented in 2007 and approved for medical use in the United States in 2011. [10] It is available as a generic medication. [11] It is on the World Health Organization's List of Essential Medicines. [12] In 2022, it was the 90th most commonly prescribed medication in the United States, with more than 7 million prescriptions. [13] [14]
Four drugs from the class of direct Xa inhibitors are marketed worldwide. Rivaroxaban (Xarelto) was the first approved FXa inhibitor to become commercially available in Europe and Canada in 2008. [1] The second one was apixaban (Eliquis), approved in Europe in 2011 [2] and in the United States in 2012. [3]
Antistasin, the first discovered naturally occurring direct Xa inhibitor Rivaroxaban, the first synthetic direct Xa inhibitor marketed as a drug Prior to the introduction of direct factor Xa inhibitors, vitamin K antagonists such as warfarin were the only oral anticoagulants for over 60 years, and together with heparin have been the main blood ...
Andexanet alfa is used to stop life-threatening or uncontrollable bleeding in people who are taking rivaroxaban or apixaban. [ 8 ] Studies in healthy volunteers show that the molecule binds factor Xa inhibitors and counters their anti-Xa-activity. [ 11 ]
Version 3.0 also included drug transporter data, drug pathway data, drug pricing, patent and manufacturing data as well as data on >5000 experimental drugs. Version 4.0 was released in 2014. [ 4 ] This version included 1558 FDA-approved small molecule drugs, 155 biotech drugs and 4200 unique drug targets.
A new drug application (NDA) for the approval of apixaban was submitted to the US Food and Drug Administration (FDA) by Bristol-Myers Squibb (BMS) and Pfizer jointly after the conclusion of the ARISTOTLE clinical trial in 2011. [29] [15] Apixaban was approved for the prevention of stroke in people with atrial fibrillation in December 2012.
Edoxaban, sold under the brand name Lixiana among others, is an anticoagulant medication and a direct factor Xa inhibitor. [3] It is taken by mouth. [3]Compared with warfarin it has fewer drug interactions.
Betrixaban (trade name Bevyxxa) is an oral anticoagulant drug which acts as a direct factor Xa inhibitor. [1] Betrixaban is FDA approved for venous thrombosis prevention in adults hospitalized for an acute illness who are at risk for thromboembolic complications. [ 2 ]