BEVYXXA ™ (betrixaban) capsule

BEVYXXA ™ (betrixaban) capsule

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BEVYXXA (betrixaban) capsule

Betrixaban, a factor Xa (FXa) inhibitor, is chemically described as N-(5-chloropyridin-2-yl)-2- [4-(N,N-dimethylcarbamimidoyl)-benzoylamino]-5-methoxybenzamide maleate. Its molecular formula (as maleate salt) is C27H26ClN5O7, which corresponds to a molecular weight of 567.98.

BEVYXXA capsules are available for oral administration in strengths of 80 mg and 40 mg of betrixaban with the following inactive ingredients: dextrose monohydrate, croscarmellose sodium, magnesium stearate, and a hard gelatin capsule.

Indications and usage

BEVYXXA is a factor Xa (FXa) inhibitor indicated for the prophylaxis of venous thromboembolism (VTE) in adult patients hospitalized for an acute medical illness who are at risk for thromboembolic complications due to moderate or severe restricted mobility and other risk factors for VTE.

Limitations of Use: Safety and efficacy of BEVYXXA have not been established in patients with prosthetic heart valves because this population has not been studied.

Mechanism of Action

Betrixaban is an oral FXa inhibitor that selectively blocks the active site of FXa and does not require a cofactor (such as Anti-thrombin III) for activity. Betrixaban inhibits free FXa and prothrombinase activity. By directly inhibiting FXa, betrixaban decreases thrombin generation (TG). Betrixaban has no direct effect on platelet aggregation.

Dosage and administration

The recommended dose of BEVYXXA is an initial single dose of 160 mg, followed by 80 mg once daily, taken at the same time each day with food. The recommended duration of treatment is 35 to 42 days.

  • Reduce dose for patients with severe renal impairment.
  • For patients receiving or starting concomitant P-gp inhibitors the recommended dose of BEVYXXA is an initial single dose of 80 mg followed by 40 mg once daily. The recommended duration of treatment is 35 to 42 days.

Missed Dose

If a dose of BEVYXXA is not taken at the scheduled time, the dose should be taken as soon as possible on the same day. The BEVYXXA dose should not be doubled to make up for a missed dose.

Contraindications

BEVYXXA is contraindicated in patients with:

  • Active pathological bleeding
  • Severe hypersensitivity reaction to betrixaban

Warnings and precautions

Risk of Bleeding

BEVYXXA increases the risk of bleeding and can cause serious and potentially fatal bleeding. Promptly evaluate any signs or symptoms of blood loss. Concomitant use of drugs affecting hemostasis increases the risk of bleeding. These include aspirin and other antiplatelet agents, other anticoagulants, heparin, thrombolytic agents, selective serotonin reuptake inhibitors, serotonin norepinephrine reuptake inhibitors, and nonsteroidal anti-inflammatory drugs (NSAIDs)

Spinal/Epidural Anesthesia or Puncture

When neuraxial anesthesia (spinal/epidural anesthesia) or spinal/epidural puncture is employed, patients treated with antithrombotic agents for prevention of thromboembolic complications are at risk of developing an epidural or spinal hematoma which can result in long-term or permanent paralysis.

Do not remove an epidural catheter earlier than 72 hours after the last administration of BEVYXXA. Do not administer the next BEVYXXA dose earlier than 5 hours after the removal of the catheter. If traumatic puncture occurs, delay the administration of TRADENAME for 72 hours.

Use in Patients with Severe Renal Impairment

Patients with severe renal impairment (CrCl ≥ 15 to < 30 mL/min computed by Cockcroft-Gault using actual body weight) taking BEVYXXA may have an increased risk of bleeding events. Reduce dose of BEVYXXA, monitor patients closely, and promptly evaluate any signs or symptoms of blood loss in these patients.

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Use in Patients on Concomitant P-gp Inhibitors

Patients on concomitant P-gp inhibitors with BEVYXXA may have an increased risk of bleeding. Reduce dose of BEVYXXA in patients receiving or starting P-gp inhibitors. Monitor patients closely and promptly evaluate any signs or symptoms of blood loss in these patients

Adverse reactions

Most common adverse reaction (incidence >5%) is bleeding.

Drug interactions

Inhibitors of P-gp: BEVYXXA is a substrate of P-gp and concomitant use of P-gp inhibitors (e.g., amiodarone, azithromycin, verapamil, ketoconazole, clarithromycin) results in an increased exposure of BEVYXXA. Reduce the dose of BEVYXXA for patients receiving or starting concomitant P-gp inhibitors.

Anticoagulants, Antiplatelets, and Thrombolytics: Co-administration of anticoagulants, antiplatelet drugs, and thrombolytics may increase the risk of bleeding. Promptly evaluate any signs or symptoms of blood loss if patients are treated concomitantly with anticoagulants, aspirin, other platelet aggregation inhibitors, and/or NSAIDs

Use in specific populations

Pregnancy: There are no data with the use of BEVYXXA in pregnant women, but treatment is likely to increase the risk of hemorrhage during pregnancy and delivery. Consider the risks of bleeding and of stroke in using BEVYXXA in this setting.

Lactation: No data are available regarding the presence of betrixaban or its metabolites in human milk, the effects of the drug on the breastfed infant, or the effects of the drug on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for BEVYXXA and any potential adverse effects on the breast-fed child from BEVYXXA or from the underlying maternal condition.

Pediatric Use: Safety and effectiveness in pediatric patients have not been established.

Geriatric Use: Of the total number of patients in the APEX clinical study 90% were 65 years and over, while 68.6% were greater than or equal to 75 years. No clinically significant differences in safety or effectiveness were observed between older and younger patients.

Renal Impairment: Patients with severe renal impairment (CrCl ≥ 15 to < 30 mL/min computed by Cockcroft-Gault using actual body weight) may have an increased risk of bleeding events. Reduce the BEVYXXA dose for patients with severe renal impairment. Monitor patients closely and promptly evaluate any signs or symptoms of blood loss in these patients.

Hepatic Impairment: BEVYXXA has not been evaluated in patients with hepatic impairment, because these patients may have intrinsic coagulation abnormalities. Therefore, the use of BEVYXXA is not recommended in patients with hepatic impairment.

Overdosage

Overdose of BEVYXXA increases the risk of bleeding. A specific reversal agent for BEVYXXA is not available. There is no experience with hemodialysis in individuals receiving betrixaban. Protamine sulfate, vitamin K, and tranexamic acid are not expected to reverse the anticoagulant activity of betrixaban.

Storage and Handling

Store at room temperature; 20°C to 25°C (68°F to 77°F)

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