Warfarin and cytochrome P450 2C9 genotype: possible ethnic variation in warfarin sensitivity

Pharmacogenomics. 2007 Mar;8(3):217-25. doi: 10.2217/14622416.8.3.217.

Abstract

Introduction: Warfarin is a widely prescribed, efficacious oral anticoagulant. S-warfarin, the more active form, is metabolized by the cytochrome P450 (CYP)2C9 enzyme. The aim was to evaluate the influence of two CYP2C9 functional polymorphisms (*2 and *3) on warfarin dose in African-Americans, an unstudied population and Caucasians, and also to assess the effect of these polymorphisms on anticoagulation response after accounting for nongenetic factors and genetic factors that might also impact the dose-response relationship of warfarin.

Patients and methods: A prospective cohort of 362 patients with a target international normalized ratio of between 2.0 and 3.0 were genotyped. Warfarin sensitivity stratified by genotype was investigated using univariate and multivariate analyses.

Results: The maintenance dose of warfarin was significantly related to genotype (p < 0.01) (variant carriers: 31.25 mg/week; wild-type: 37.5 mg/week), even after adjustment for possible confounding factors (p = 0.046). However, the effect of genotype was restricted to Caucasians, in whom variant carriers had a significantly lower maintenance dose compared with wild-type homozygotes (unadjusted: p < 0.01; adjusted: p = 0.02). There was a greater risk of over-anticoagulation among Caucasian variant carriers, although this was only observed prior to reaching maintenance dose. For African-American variant carriers, there was no difference in warfarin response based on CYP2C9 genotype.

Discussion: CYP2C9 *2 and *3 variants provide predictive information in anticoagulation response. However, these variants may not be useful in African-Americans or as a marker of long-term over-anticoagulation once a stable dose is reached.

Publication types

  • Comparative Study
  • Research Support, N.I.H., Extramural

MeSH terms

  • Adult
  • Aged
  • Anticoagulants / adverse effects
  • Anticoagulants / therapeutic use*
  • Aryl Hydrocarbon Hydroxylases / genetics*
  • Black or African American / genetics*
  • Cohort Studies
  • Cytochrome P-450 CYP2C9
  • Female
  • Gene Frequency / genetics
  • Genetic Variation / genetics*
  • Genotype
  • Humans
  • International Normalized Ratio
  • Male
  • Middle Aged
  • Prospective Studies
  • Warfarin / adverse effects
  • Warfarin / therapeutic use*
  • White People / genetics*

Substances

  • Anticoagulants
  • Warfarin
  • CYP2C9 protein, human
  • Cytochrome P-450 CYP2C9
  • Aryl Hydrocarbon Hydroxylases