VKORC1 and CYP2C9 allelic variants influence acenocoumarol dose requirements in Greek patients

Pharmacogenomics. 2008 Nov;9(11):1631-8. doi: 10.2217/14622416.9.11.1631.

Abstract

Aim: To identify the frequencies of the polymorphisms CYP2C9*2, CYP2C9*3 and VKORC1-1639 G>A in the Greek population and investigate whether these polymorphisms and patient demographics (age, sex and comedication) could explain the interindividual variability of acenocoumarol dose requirements for efficient anticoagulation.

Materials & methods: CYP2C9*2 (Arg144Cys), CYP2C9*3 (Ile359Leu) and VKORC1-1639G>A allelic variants were analyzed in 98 patients treated with acenocoumarol.

Results: Allelic frequencies of CYP2C9*2, CYP2C9*3 and VKORC1A were found to be 0.155, 0.075 and 0.485, respectively. Carriership of at least one CYP2C9*3 allele led to the most pronounced reduction in the required mean dose (p<0.0001). In contrast, the CYP2C9*2 allele played a minor role (p=0.3). VKORC1 A/A patients needed approximately a third of the dose required by wild-type patients to achieve the target INR (p<0.0001). Age was the only demographical factor significantly affecting acenocoumarol dose (p<0.0001). In a multivariable regression model, CYP2C9, VKORC1 genotypes and age explained 55% of acenocoumarol dosing variability.

Conclusion: VKORC1-1639G>A, CYP2C9*2 and CYP2C9*3 polymorphisms were found to predispose to acenocoumarol sensitivity in Greeks. Other hereditary and nongenetic parameters must be incorporated in an individualized dosing algorithm to achieve a safer anticoagulant effect.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acenocoumarol / administration & dosage*
  • Acenocoumarol / pharmacokinetics
  • Acenocoumarol / therapeutic use
  • Anticoagulants / administration & dosage*
  • Anticoagulants / pharmacokinetics
  • Anticoagulants / therapeutic use
  • Aryl Hydrocarbon Hydroxylases / genetics*
  • Cohort Studies
  • Cytochrome P-450 CYP2C9
  • Dose-Response Relationship, Drug
  • Female
  • Gene Frequency
  • Greece
  • Humans
  • Male
  • Middle Aged
  • Mixed Function Oxygenases / genetics*
  • Polymorphism, Single Nucleotide*
  • Pulmonary Embolism / genetics
  • Pulmonary Embolism / prevention & control
  • Regression Analysis
  • Retrospective Studies
  • Venous Thrombosis / genetics
  • Venous Thrombosis / prevention & control
  • Vitamin K Epoxide Reductases

Substances

  • Anticoagulants
  • Mixed Function Oxygenases
  • CYP2C9 protein, human
  • Cytochrome P-450 CYP2C9
  • Aryl Hydrocarbon Hydroxylases
  • VKORC1 protein, human
  • Vitamin K Epoxide Reductases
  • Acenocoumarol