CYP2C19 genotype predicts steady state escitalopram concentration in GENDEP

J Psychopharmacol. 2012 Mar;26(3):398-407. doi: 10.1177/0269881111414451. Epub 2011 Sep 17.

Abstract

In vitro work shows CYP2C19 and CYP2D6 contribute to the metabolism of escitalopram to its primary metabolite, N-desmethylescitalopram. We report the effect of CYP2C19 and CYP2D6 genotypes on steady state morning concentrations of escitalopram and N-desmethylescitalopram and the ratio of this metabolite to the parent drug in 196 adult patients with depression in GENDEP, a clinical pharmacogenomic trial. Subjects who had one CYP2D6 allele associated with intermediate metabolizer phenotype and one associated with poor metabolizer (i.e. IM/PM genotypic category) had a higher mean logarithm escitalopram concentration than CYP2D6 extensive metabolizers (EMs) (p = 0.004). Older age was also associated with higher concentrations of escitalopram. Covarying for CYP2D6 and age, we found those homozygous for the CYP2C19*17 allele associated with ultrarapid metabolizer (UM) phenotype had a significantly lower mean escitalopram concentration (2-fold, p = 0.0001) and a higher mean metabolic ratio (p = 0.0003) than EMs, while those homozygous for alleles conferring the PM phenotype had a higher mean escitalopram concentration than EMs (1.55-fold, p = 0.008). There was a significant overall association between CYP2C19 genotypic category and escitalopram concentration (p = 0.0003; p = 0.0012 Bonferroni corrected). In conclusion, we have demonstrated an association between CYP2C19 genotype, including the CYP2C19*17 allele, and steady state escitalopram concentration.

Publication types

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

MeSH terms

  • Adult
  • Aged
  • Antidepressive Agents / blood*
  • Antidepressive Agents / pharmacokinetics
  • Antidepressive Agents / therapeutic use
  • Aryl Hydrocarbon Hydroxylases / genetics*
  • Aryl Hydrocarbon Hydroxylases / metabolism
  • Biotransformation
  • Citalopram / analogs & derivatives
  • Citalopram / blood*
  • Citalopram / pharmacokinetics
  • Citalopram / therapeutic use
  • Cytochrome P-450 CYP2C19
  • Cytochrome P-450 CYP2D6 / genetics
  • Cytochrome P-450 CYP2D6 / metabolism
  • Depressive Disorder, Major / blood*
  • Depressive Disorder, Major / drug therapy*
  • Depressive Disorder, Major / genetics
  • Depressive Disorder, Major / metabolism
  • Diagnostic and Statistical Manual of Mental Disorders
  • Female
  • Genetic Association Studies
  • Genotype
  • Humans
  • Male
  • Middle Aged
  • Polymorphism, Genetic*
  • Selective Serotonin Reuptake Inhibitors / blood*
  • Selective Serotonin Reuptake Inhibitors / pharmacokinetics
  • Selective Serotonin Reuptake Inhibitors / therapeutic use
  • White People
  • Young Adult

Substances

  • Antidepressive Agents
  • Serotonin Uptake Inhibitors
  • Citalopram
  • desmethylcitalopram
  • Aryl Hydrocarbon Hydroxylases
  • CYP2C19 protein, human
  • Cytochrome P-450 CYP2C19
  • Cytochrome P-450 CYP2D6

Associated data

  • ISRCTN/ISRCTN03693000