Safety, tolerability, pharmacodynamics, and pharmacokinetics of rivaroxaban--an oral, direct factor Xa inhibitor--are not affected by aspirin

J Clin Pharmacol. 2006 Sep;46(9):981-90. doi: 10.1177/0091270006292127.

Abstract

Rivaroxaban (BAY 59-7939) is an oral, direct Factor Xa inhibitor in advanced clinical development for the prevention and treatment of thromboembolic disorders. This was a randomized, 2-way crossover study in healthy male subjects, with an aspirin run-in period, to examine whether aspirin influences the safety, tolerability, pharmacodynamics, and pharmacokinetics of rivaroxaban. All treatments were well tolerated; drug-related adverse events were mild and transient. Aspirin did not alter the effects of rivaroxaban on Factor Xa activity or clotting tests. Platelet aggregation and bleeding time were not affected by rivaroxaban, and rivaroxaban did not influence the effects of aspirin on these parameters to a clinically relevant extent. Aspirin did not affect the pharmacokinetics of rivaroxaban, including the fraction unbound. This study suggests that there is no clinically relevant interaction between rivaroxaban and aspirin and that the 2 drugs could be administered concomitantly at the doses used in this study.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Administration, Oral
  • Adolescent
  • Adult
  • Antithrombin III
  • Aspirin / pharmacology*
  • Bleeding Time
  • Dose-Response Relationship, Drug
  • Drug Tolerance*
  • Humans
  • Male
  • Middle Aged
  • Molecular Structure
  • Morpholines / administration & dosage
  • Morpholines / adverse effects
  • Morpholines / pharmacokinetics*
  • Morpholines / pharmacology*
  • Platelet Aggregation / drug effects
  • Rivaroxaban
  • Thiophenes / administration & dosage
  • Thiophenes / adverse effects
  • Thiophenes / pharmacokinetics*
  • Thiophenes / pharmacology*

Substances

  • Morpholines
  • Thiophenes
  • Antithrombin III
  • Rivaroxaban
  • Aspirin