Products
Betrixaban was approved in the United States in 2017 in capsule form (Bevyxxa). The drug has not yet been approved in the EU (Dexxience).
Structure and properties
Betrixaban (C23H22ClN5O3, Mr = 451.9 g/mol) is present in the drug as betrixaban maleate. It is a pyridine and anthranilamide derivative.
Effects
Betrixaban has antithrombotic properties. The effects are due to direct, reversible, and selective inhibition of factor Xa. This coagulation factor plays an important role in the blood clotting cascade. It is a serine protease formed from factor X in both the intrinsic and extrinsic pathways and catalyzes the formation of thrombin from prothrombin. Thrombin converts fibrinogen to fibrin, promoting the formation of the fibrin plug. Factor Xa inhibitors additionally have an indirect effect on platelet aggregation. Betrixaban has a long half-life of 19 to 27 hours. Unlike heparins, factor Xa inhibitors do not need to be injected under the skin but can be taken perorally. Compared with vitamin K antagonists such as phenprocoumon, they have predictable and linear pharmacokinetics and a rapid onset of action. Dosing is simple (fixed) and no therapy monitoring is required.
Indications
For the prevention of deep vein thrombosis and pulmonary embolism in hospitalized adults with acute illness who are at risk for these complications because of severely limited mobility or other factors.
Dosage
According to the SmPC. Capsules are taken once daily with food.
Contraindications
- Hypersensitivity
- Active bleeding
For complete precautions, see the drug label.
Interactions
Betrixaban is a substrate of P-glycoprotein and interactions with P-gp inhibitors are possible. Caution is advised when combining it with drugs that affect blood clotting. These include, for example, nonsteroidal anti-inflammatory drugs, acetylsalicylic acid, antiplatelet drugs, and vitamin K antagonists.
Adverse effects
The most common potential adverse effects include bleeding in various organs.
