Effect of CYP2C19*2 and *17 genetic variants on platelet response to clopidogrel and prasugrel maintenance dose and relation to bleeding complications

Am J Cardiol. 2013 Apr 1;111(7):985-90. doi: 10.1016/j.amjcard.2012.12.013. Epub 2013 Jan 19.

Abstract

The present study was performed to compare the influence of cytochrome P459 2C19 (CYP2C19) *2 and *17 genetic variants on the platelet response to clopidogrel and prasugrel maintenance therapy and to assess the relation between platelet reactivity and bleeding complications. A total of 730 patients were included (517 patients treated with clopidogrel 150 mg/day and 213 discharged with prasugrel 10 mg). Platelet reactivity was assessed at 1 month with the platelet reactivity index vasodilator-stimulated phosphoprotein (PRI VASP). High on-treatment platelet reactivity was defined as PRI VASP >50% and low on-treatment platelet reactivity (LTPR) as PRI VASP <20%. The patients were classified according to their genotypes as poor metabolizers (*2/non *17), intermediate metabolizers (*2/*17 or non *2/non *17) and ultrametabolizers (non *2/*17). At 1 month, the prasugrel response was significantly better than the clopidogrel response in all groups of patients, with a lower incidence of high on-treatment platelet reactivity but a greater incidence of LTPR, regardless of the genetic variants. The genetic distribution had a significant effect on the mean PRI VASP values, the incidence of high on-treatment platelet reactivity, and LTPR with both clopidogrel and prasugrel (p <0.05 for all). LTPR identified a group of patients at a greater risk of bleeding (odds ratio 4.8, 95% confidence interval 2.7 to 8.3; p <0.0001). In conclusion, the present study showed that both clopidogrel and prasugrel have genetic modulation by CYP2C19 *2 and *17 alleles and that prasugrel provides greater platelet inhibition, regardless of the genotypes. In addition, LTPR was associated with a greater risk of bleeding.

MeSH terms

  • Acute Coronary Syndrome / drug therapy*
  • Acute Coronary Syndrome / genetics*
  • Acute Coronary Syndrome / metabolism
  • Alleles
  • Aryl Hydrocarbon Hydroxylases / genetics*
  • Blood Platelets / drug effects*
  • Cell Adhesion Molecules
  • Clopidogrel
  • Cytochrome P-450 CYP2C19
  • Female
  • Genetic Variation
  • Genotype
  • Hemorrhage / genetics*
  • Humans
  • Male
  • Microfilament Proteins
  • Middle Aged
  • Myocardial Infarction / drug therapy*
  • Myocardial Infarction / genetics*
  • Myocardial Infarction / metabolism
  • Phosphoproteins
  • Piperazines / administration & dosage
  • Piperazines / therapeutic use*
  • Polymerase Chain Reaction
  • Prasugrel Hydrochloride
  • Prospective Studies
  • Purinergic P2Y Receptor Antagonists / administration & dosage
  • Purinergic P2Y Receptor Antagonists / therapeutic use*
  • Risk Factors
  • Thiophenes / administration & dosage
  • Thiophenes / therapeutic use*
  • Ticlopidine / administration & dosage
  • Ticlopidine / analogs & derivatives*
  • Ticlopidine / therapeutic use
  • Treatment Outcome

Substances

  • Cell Adhesion Molecules
  • Microfilament Proteins
  • Phosphoproteins
  • Piperazines
  • Purinergic P2Y Receptor Antagonists
  • Thiophenes
  • vasodilator-stimulated phosphoprotein
  • Clopidogrel
  • Aryl Hydrocarbon Hydroxylases
  • CYP2C19 protein, human
  • Cytochrome P-450 CYP2C19
  • Prasugrel Hydrochloride
  • Ticlopidine