Betrixaban API Manufacturers

General Description:

Betrixaban, identified by CAS number 330942-05-7, is a notable compound with significant therapeutic applications. Betrixaban is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa . It was selected among all lead compounds due to its low hERG channel affinity while sustaining its factor Xa inhibition capacity . Betrixaban, now developed by Portola Pharmaceuticals Inc, is prescribed as a venous thromboembolism (VTE) prophylactic for adult patients with moderate to severe restricted motility or with other risks for VTE . VTE can be manifested as deep vein thrombosis or pulmonary embolism and it is a leading cause of preventable death in hospitalized patients .

Indications:

This drug is primarily indicated for: Betrixaban is indicated for prophylaxis of venous thromboembolism (VTE) in conditions of moderate to severe restricted mobility or in patients that qualify as in risk of VTE. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Betrixaban undergoes metabolic processing primarily in: One of the major characteristics of Betrixaban is its minimal hepatic metabolism (< 1%), preventing potential accumulation with liver impariment. Unchanged Betrixaban is the main form found in human plasma, followed by two hydolitic CYP-independent inactive metabolites (15-18%). The minimal hepatic metabolism produces an unlikely drug-to-drug interaction with inhibitors or agonists of CYP450 . This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Betrixaban are crucial for its therapeutic efficacy: Betrixaban presents a rapid absorption at a dose of 80 mg. Its peak plasma concentration is registered within 3-4 hours after oral administration in healthy humans. The oral bioavailability is 34%, and it can be reduced with the consumption of food. Specifically, the C_max and AUC is reduced by an average of 70% and 61% with a low-fat meal, and 50% and 48% with a high-fat meal compared to the fasted state, an effect which is apparent up to six hours following food intake. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Betrixaban is an important consideration for its dosing schedule: Betrixaban presents a long half-life of between 19-27 hours . This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Betrixaban exhibits a strong affinity for binding with plasma proteins: Betrixaban is reported to be present a proteing binding of about 60% . This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Betrixaban from the body primarily occurs through: Betrixaban is reported to present mainly a gastrointestinal elimination route, it has been shown that even 85% of it gets disposed in the feces and only 11% of it can be found in the urine . Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Betrixaban is distributed throughout the body with a volume of distribution of: The apparent volume of distribution os 32 L/kg . This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Betrixaban is a critical factor in determining its safe and effective dosage: Betrixaban presents a minimal renal clearance (being 5-7% of the administered dose) . It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Betrixaban exerts its therapeutic effects through: Betrixaban is an oral anticoagulant that excerts its action by preventing thrombin generation without having a direct effect on platelet aggregation . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Betrixaban functions by: Betrixaban is a cofactor-independent direct inhibitor of the Factor Xa and inhibits free and prothrombinase-bound Factor Xa . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Betrixaban belongs to the class of organic compounds known as benzanilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with a benzene ring. They have the general structure RNC(=O)R', where R,R'= benzene, classified under the direct parent group Benzanilides. This compound is a part of the Organic compounds, falling under the Benzenoids superclass, and categorized within the Benzene and substituted derivatives class, specifically within the Anilides subclass.

Categories:

Betrixaban is categorized under the following therapeutic classes: Acids, Carbocyclic, Amides, Anticoagulants, Antithrombins, Benzene Derivatives, Benzoates, Blood and Blood Forming Organs, Direct factor Xa inhibitors, Enzyme Inhibitors, Factor Xa Inhibitors, Hematologic Agents, P-glycoprotein substrates, Protease Inhibitors, Serine Protease Inhibitors. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Betrixaban include:

• Water Solubility: 2.5-2.7 mg/ml
• Melting Point: 200-212 ºC