BAY 59-7939: an oral, direct factor Xa inhibitor for the prevention of venous thromboembolism in patients after total knee replacement. A phase II dose-ranging study

J Thromb Haemost. 2005 Nov;3(11):2479-86. doi: 10.1111/j.1538-7836.2005.01602.x.

Abstract

Background: BAY 59-7939, a novel, oral, direct factor Xa inhibitor, is in clinical development for the prevention of venous thromboembolism (VTE), a frequent complication following orthopaedic surgery.

Methods: In a multicenter, parallel-group, double-blind, double-dummy study, 621 patients undergoing elective total knee replacement were randomly assigned to oral BAY 59-7939 (2.5, 5, 10, 20, and 30 mg b.i.d., initiated 6-8 h postsurgery), or subcutaneous enoxaparin (30 mg b.i.d., initiated 12-24 h postsurgery). Treatment was continued until mandatory bilateral venography 5-9 days after surgery. The primary efficacy endpoint was a composite of any deep vein thrombosis (proximal and/or distal), confirmed non-fatal pulmonary embolism and all-cause mortality during treatment. The primary safety endpoint was major, postoperative bleeding during treatment.

Results: Of the 613 patients treated, 366 (59.7%) were evaluable for the primary efficacy analysis. The primary efficacy endpoint occurred in 31.7%, 40.4%, 23.3%, 35.1%, and 25.4% of patients receiving 2.5, 5, 10, 20 and 30 mg b.i.d. doses of BAY 59-7939, respectively (test for trend, P = 0.29), compared with 44.3% in the enoxaparin group. The frequency of major, postoperative bleeding increased with increasing doses of BAY 59-7939 (test for trend, P = 0.0007), with no significant difference between any dose group compared with enoxaparin. Bleeding endpoints were lower for the 2.5-10 mg b.i.d. doses compared with higher doses of BAY 59-7939.

Conclusions: Oral administration of 2.5-10 mg b.i.d. of BAY 59-7939, early in the postoperative period, showed potential efficacy and an acceptable safety profile, similar to enoxaparin, for the prevention of VTE in patients undergoing elective total knee replacement.

Publication types

  • Clinical Trial, Phase II
  • Comparative Study
  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Adult
  • Aged
  • Aged, 80 and over
  • Anticoagulants / administration & dosage
  • Anticoagulants / adverse effects
  • Anticoagulants / therapeutic use
  • Antithrombin III / administration & dosage
  • Antithrombin III / adverse effects
  • Antithrombin III / therapeutic use*
  • Arthroplasty, Replacement, Knee / adverse effects*
  • Double-Blind Method
  • Enoxaparin / administration & dosage
  • Enoxaparin / adverse effects
  • Enoxaparin / therapeutic use
  • Hemorrhage / epidemiology*
  • Hemorrhage / etiology
  • Humans
  • Incidence
  • Injections, Subcutaneous
  • Male
  • Middle Aged
  • Morpholines / administration & dosage
  • Morpholines / adverse effects
  • Morpholines / therapeutic use*
  • Rivaroxaban
  • Thiophenes / administration & dosage
  • Thiophenes / adverse effects
  • Thiophenes / therapeutic use*
  • Thromboembolism / epidemiology
  • Thromboembolism / etiology*
  • Thromboembolism / prevention & control*
  • Venous Thrombosis / epidemiology
  • Venous Thrombosis / etiology*
  • Venous Thrombosis / prevention & control*

Substances

  • Anticoagulants
  • Enoxaparin
  • Morpholines
  • Thiophenes
  • Antithrombin III
  • Rivaroxaban