Genetics and clinical response to warfarin and edoxaban in patients with venous thromboembolism

Heart. 2017 Nov;103(22):1800-1805. doi: 10.1136/heartjnl-2016-310901. Epub 2017 Jul 8.

Abstract

Objective: The aim of this study was to investigate whether genetic variants can identify patients with venous thromboembolism (VTE) at an increased risk of bleeding with warfarin.

Methods: Hokusai-venous thromboembolism (Hokusai VTE), a randomised, multinational, double-blind, non-inferiority trial, evaluated the safety and efficacy of edoxaban versus warfarin in patients with VTE initially treated with heparin. In this subanalysis of Hokusai VTE, patients genotyped for variants in CYP2C9 and VKORC1 genes were divided into three warfarin sensitivity types (normal, sensitive and highly sensitive) based on their genotypes. An exploratory analysis was also conducted comparing normal responders to pooled sensitive responders (ie, sensitive and highly sensitive responders).

Results: The analysis included 47.7% (3956/8292) of the patients in Hokusai VTE. Among 1978 patients randomised to warfarin, 63.0% (1247) were normal responders, 34.1% (675) were sensitive responders and 2.8% (56) were highly sensitive responders. Compared with normal responders, sensitive and highly sensitive responders had heparin therapy discontinued earlier (p<0.001), had a decreased final weekly warfarin dose (p<0.001), spent more time overanticoagulated (p<0.001) and had an increased bleeding risk with warfarin (sensitive responders HR 1.38 [95% CI 1.11 to 1.71], p=0.0035; highly sensitive responders 1.79 [1.09 to 2.99]; p=0.0252).

Conclusion: In this study, CYP2C9 and VKORC1 genotypes identified patients with VTE at increased bleeding risk with warfarin.

Trial registration number: NCT00986154.

Keywords: CYP2C9; VKORC1; edoxaban; venous thromboembolism; warfarin sensitivity.

Publication types

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

MeSH terms

  • Adult
  • Aged
  • Anticoagulants / adverse effects*
  • Blood Coagulation / drug effects*
  • Cytochrome P-450 CYP2C9 / genetics*
  • Cytochrome P-450 CYP2C9 / metabolism
  • Double-Blind Method
  • Drug Monitoring
  • Factor Xa Inhibitors / adverse effects*
  • Female
  • Genetic Predisposition to Disease
  • Hemorrhage / chemically induced
  • Hemorrhage / diagnosis
  • Hemorrhage / genetics*
  • Humans
  • Male
  • Middle Aged
  • Pharmacogenetics
  • Pharmacogenomic Variants*
  • Phenotype
  • Pyridines / adverse effects*
  • Risk Assessment
  • Risk Factors
  • Thiazoles / adverse effects*
  • Time Factors
  • Treatment Outcome
  • Venous Thromboembolism / blood
  • Venous Thromboembolism / diagnosis
  • Venous Thromboembolism / drug therapy*
  • Venous Thromboembolism / genetics
  • Vitamin K Epoxide Reductases / genetics*
  • Vitamin K Epoxide Reductases / metabolism
  • Warfarin / adverse effects*

Substances

  • Anticoagulants
  • Factor Xa Inhibitors
  • Pyridines
  • Thiazoles
  • Warfarin
  • CYP2C9 protein, human
  • Cytochrome P-450 CYP2C9
  • VKORC1 protein, human
  • Vitamin K Epoxide Reductases
  • edoxaban

Associated data

  • ClinicalTrials.gov/NCT00986154