CYP2D6 -1584C>G promoter polymorphism and debrisoquine ultrarapid hydroxylation in healthy volunteers

Pharmacogenomics. 2013 Dec;14(16):1973-7. doi: 10.2217/pgs.13.181.

Abstract

Background & aim: The CYP2D6 -1584C>G polymorphism (rs1080985) has been identified as a major factor for CYP2D6 expression and function, with the mutant -1584G promoter type being consistently associated with significantly greater expression than -1584C. It may therefore be associated with ultrarapid metabolism. The objective of the present study was to explore the relationship between the CYP2D6 -1584C>G polymorphism and the debrisoquine metabolic ratio in healthy volunteers in order to evaluate its potential impact on the ultrarapid CYP2D6 hydroxylation capacity.

Materials & methods: The CYP2D6 -1584C>G polymorphism was analyzed in 320 unrelated healthy individuals who were previously phenotyped for debrisoquine hydroxylation.

Results: The metabolic ratio (log10 mean ± standard deviation) of individuals with the -1584G allele was lower than that of individuals with the -1584C allele for carriers of one active CYP2D6 gene (-0.13 ± 0.33 and 0.17 ± 0.52, respectively; p < 0.05) or two active CYP2D6 genes (-0.32 ± 0.39 and -0.20 ± 0.44, respectively; p < 0.05).

Conclusion: The presence of the -1584G allele in the promoter region of the CYP2D6 gene was related to a high CYP2D6 hydroxylation capacity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alleles
  • Cytochrome P-450 CYP2D6 / genetics*
  • Debrisoquin / therapeutic use*
  • Gene Expression Regulation / drug effects
  • Genotype
  • Healthy Volunteers
  • Heterozygote
  • Humans
  • Hydroxylation / drug effects
  • Hydroxylation / genetics*
  • Polymorphism, Genetic
  • Promoter Regions, Genetic

Substances

  • Cytochrome P-450 CYP2D6
  • Debrisoquin