Betrixaban (trade name Bevyxxa) is an oral anticoagulant drug which acts as a

direct factor Xa inhibitor Direct may refer to: Mathematics * Directed set, in order theory * Direct limit of (pre), sheaves * Direct sum of modules, a construction in abstract algebra which combines several vector spaces Computing * Direct access (disambiguation), a ...

. 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 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 lungs to ...

prevention in adults hospitalized for an

acute Acute may refer to: Science and technology * Acute angle ** Acute triangle ** Acute, a leaf shape in the glossary of leaf morphology * Acute (medicine), a disease that it is of short duration and of recent onset. ** Acute toxicity, the adverse eff ...

illness who are at risk for thromboembolic complications. Compared to other directly acting oral anticoagulants betrixaban has relatively low

renal excretion In pharmacology, clearance is a pharmacokinetics, pharmacokinetic measurement of the volume of blood plasma, plasma from which a substance is completely removed per unit time. Usually, clearance is measured in L/h or mL/min. The quantity reflects t ...

and is not metabolized by CYP3A4.

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 act ...

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 i ...

acquired rights for betrixaban in 2004 and co-developed it with

Merck Merck refers primarily to the German Merck family and three companies founded by the family, including: * the Merck Group, a German chemical, pharmaceutical and life sciences company founded in 1668 ** Merck Serono (known as EMD Serono in the Unite ...

. In 2011 Merck discontinued joint development. The drug has undergone clinical trials for prevention of embolism after knee surgery and for prevention of stroke following non-valvular atrial fibrillation. 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. Specifically it i ...

and

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

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

References

Direct Xa inhibitors {{blood-drug-stub

History

See also

References