Efficacy and safety of the oral direct factor Xa inhibitor apixaban for symptomatic deep vein thrombosis. The Botticelli DVT dose-ranging study

J Thromb Haemost. 2008 Aug;6(8):1313-8. doi: 10.1111/j.1538-7836.2008.03054.x. Epub 2008 Jun 6.

Abstract

Background: Apixaban, an oral potent reversible direct inhibitor of activated factor X, has shown promise in the prevention of venous thromboembolism following major orthopedic surgery. We conducted a dose-ranging study in patients with deep vein thrombosis.

Methods: Consecutive patients with symptomatic deep vein thrombosis were included and randomized to receive 84-91 days of apixaban 5 mg twice-daily, 10 mg twice-daily, or 20 mg once-daily, or low molecular weight heparin (LMWH) followed by a vitamin K antagonist (VKA). The primary efficacy outcome was the composite of symptomatic recurrent venous thromboembolism and asymptomatic deterioration of bilateral compression ultrasound or perfusion lung scan. The principal safety outcome was the composite of major and clinically relevant, non-major bleeding.

Results: The mean age of the 520 included patients was 59 years, and 62% were male. The primary outcome occurred in 17 of the 358 apixaban-treated patients [4.7%, 95% confidence interval (CI) 2.8-7.5%] and in five of the 118 LMWH/VKA-treated patients (4.2%, 95% CI 1.4-9.6%) who were evaluable. The incidence in all three apixaban groups was low and comparable without evidence of a dose response. The principal safety outcome occurred in 28 (7.3%) of the 385 apixaban-treated patients and in 10 (7.9%) of the 126 LMWH/VKA-treated patients. No dose response for apixaban was observed.

Conclusion: These observations warrant further evaluation of apixaban in phase III studies. The attractive fixed-dose regimen of this compound may meet the demand to simplify anticoagulant treatment in patients with established venous thromboembolism.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Adult
  • Aged
  • Anticoagulants / administration & dosage
  • Dose-Response Relationship, Drug
  • Double-Blind Method
  • Factor Xa Inhibitors*
  • Female
  • Fibrinolytic Agents / administration & dosage*
  • Fibrinolytic Agents / adverse effects
  • Hemorrhage / etiology
  • Heparin, Low-Molecular-Weight / administration & dosage
  • Humans
  • Male
  • Middle Aged
  • Pyrazoles / administration & dosage*
  • Pyrazoles / adverse effects
  • Pyridones / administration & dosage*
  • Pyridones / adverse effects
  • Recurrence
  • Safety
  • Treatment Outcome
  • Venous Thrombosis / drug therapy*
  • Vitamin K / antagonists & inhibitors

Substances

  • Anticoagulants
  • Factor Xa Inhibitors
  • Fibrinolytic Agents
  • Heparin, Low-Molecular-Weight
  • Pyrazoles
  • Pyridones
  • Vitamin K
  • apixaban