Betrixaban (trade name Bevyxxa) is an oral

anticoagulant An anticoagulant, commonly known as a blood thinner, is a chemical substance that prevents or reduces the coagulation of blood, prolonging the clotting time. Some occur naturally in blood-eating animals, such as leeches and mosquitoes, which ...

drug which acts as a

direct factor Xa inhibitor Direct factor Xa inhibitors (xabans) are anticoagulants (blood thinning drugs), used to both treat and prevent blood clots in veins, and prevent stroke and embolism in people with atrial fibrillation (AF). Medical use Direct factor Xa inhibitor ...

. Betrixaban is

FDA The United States Food and Drug Administration (FDA or US FDA) is a federal agency of the Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food ...

approved for

venous thrombosis Venous thrombosis is the blockage of a vein caused by a thrombus (blood clot). A common form of venous thrombosis is deep vein thrombosis (DVT), when a blood clot forms in the deep veins. If a thrombus breaks off ( embolizes) and flows to the lu ...

prevention in adults hospitalized for an acute illness who are at risk for thromboembolic complications. Compared to other

directly acting oral anticoagulants An anticoagulant, commonly known as a blood thinner, is a chemical substance that prevents or reduces the coagulation of blood, prolonging the clotting time. Some occur naturally in hematophagy, blood-eating animals, such as leeches and mosquito ...

betrixaban has relatively low renal excretion and is not metabolized by

CYP3A4 Cytochrome P450 3A4 (abbreviated CYP3A4) () is an important enzyme in the body, mainly found in the liver and in the intestine, which in humans is encoded by ''CYP3A4'' gene. It organic redox reaction, oxidizes small foreign organic molecules ( ...

History

Betrixaban was originally developed by

Millennium Pharmaceuticals Takeda Oncology (originally Millennium Pharmaceuticals) is a biopharmaceutical company based in Cambridge, Massachusetts. It is a fully owned subsidiary of Takeda Pharmaceutical. Takeda Oncology's research, development and commercialization ac ...

Portola Pharmaceuticals Portola Pharmaceuticals is an American clinical stage biotechnology company that researches, develops, and commercializes drugs. The company focuses primarily on drugs used in the treatment of thrombosis and hematological malignancies. Founded ...

acquired rights for betrixaban in 2004 and co-developed it with Merck. In 2011 Merck discontinued joint development. The drug has undergone

clinical trials Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...

for prevention of embolism after

knee In humans and other primates, the knee joins the thigh with the leg and consists of two joints: one between the femur and tibia (tibiofemoral joint), and one between the femur and patella (patellofemoral joint). It is the largest joint in the hu ...

surgery and for prevention of

stroke Stroke is a medical condition in which poor cerebral circulation, blood flow to a part of the brain causes cell death. There are two main types of stroke: brain ischemia, ischemic, due to lack of blood flow, and intracranial hemorrhage, hemor ...

following non-valvular

atrial fibrillation Atrial fibrillation (AF, AFib or A-fib) is an Heart arrhythmia, abnormal heart rhythm (arrhythmia) characterized by fibrillation, rapid and irregular beating of the Atrium (heart), atrial chambers of the heart. It often begins as short periods ...

. Betrixaban was also studied in a large phase III clinical trial for extended duration thromboprophylaxis in acute ill patients. Previously

apixaban Apixaban, sold under the brand name Eliquis, is an anticoagulant medication used to treat and prevent blood clots and to prevent stroke in people with nonvalvular atrial fibrillation through directly inhibiting factor Xa. It is used as an al ...

and

rivaroxaban Rivaroxaban, sold under the brand name Xarelto among others, is an anticoagulant medication (blood thinner) used to treat and reduce the risk of blood clots. Specifically it is used to treat deep vein thrombosis and pulmonary emboli and prev ...

have failed to show positive risk/benefit ratio in this indication compared to

enoxaparin Enoxaparin sodium, sold under the brand name Lovenox among others, is an anticoagulant medication (blood thinner). It is used to treat and prevent deep vein thrombosis (DVT) and pulmonary embolism (PE) including during pregnancy and following c ...

. APEX trial compared betrixaban with

and included 7513 patients. Lower rate of VTE events was found in betrixaban arm with no increase in major bleedings compared to enoxaparin. Based on these results betrixaban was approved by FDA on June 23, 2017, becoming the first DOAC approved for extended prophylaxis in hospitalized patients. Betrixaban has been also reviewed by

EMA Ema or EMA may refer to: Biology and medicine * Anti-Endomysial Antibodies test * Epithelial membrane antigen * European Medicines Agency, a European Union agency for the evaluation of medicinal products * European Medical Association, associa ...

but didn't receive marketing approval in EU mainly due to concerns of increased bleeding risk and absence of reversal agent.

References

{{Antithrombotics Direct Xa inhibitors 2-Aminopyridines Amides Amidines Benzene derivatives Chloropyridines Methoxy compounds

History

See also

References