Switching from prasugrel to clopidogrel based on Cytochrome P450 2C19 genotyping in East Asian patients stabilized after acute myocardial infarction

Platelets. 2016 Jun;27(4):301-7. doi: 10.3109/09537104.2015.1095875. Epub 2015 Nov 10.

Abstract

To evaluate the pharmacodynamic efficacy of de-escalating P2Y12 inhibition from prasugrel to clopidogrel based on cytochrome P450 (CYP) 2C19 genotyping, we genotyped 50 Korean patients with AMI who underwent percutaneous coronary intervention (PCI) for CYP2C19 *2,*3, or *17 using real-time PCR. They were discharged on prasugrel 10 mg daily. A control group of 48 AMI patients who underwent PCI and were discharged on clopidogrel but did not undergo genotyping was identified retrospectively. Based on genotyping results available at 3 weeks, 12 patients found to have 2 copies of either CYP2C19 *2 or *3 loss of function alleles continued prasugrel while the remaining 38 patients switched to clopidogrel 75 mg daily. The rate of patients within the therapeutic window (TW) of on-treatment platelet reactivity (OPR), 85<P2Y12 reactivity unit (PRU) ≤275, was compared in the genotype-directed cohort before (3 weeks) and after genotype-directed antiplatelet treatment (5 weeks), as well as with the control cohort at 5 weeks. In the genotype-directed group, there was an increase in the proportion of patients within the TW after genotype-directed antiplatelet treatment (48-76%, p=0.007), primarily driven by a decrease of patients with PRU <85 (52-16%, p <0.001). The proportion of patients within the TW was similar between the genotype-guided and control groups (76% vs. 72.9% p=0.726). In conclusion, individualized antiplatelet regimens based on CYP2C19 genotyping may improve likelihood of achieving a TW of OPR compared to fixed dose of prasugrel 10 mg during maintenance periods of AMI in East Asians.

Keywords: Clopidogrel; myocardial infarction; pharmacogenetics; prasugrel.

MeSH terms

  • Aged
  • Alleles
  • Asian People / genetics
  • Blood Platelets / drug effects
  • Blood Platelets / metabolism
  • Clopidogrel
  • Cytochrome P-450 CYP2C19 / genetics*
  • Drug Substitution*
  • Female
  • Genotype*
  • Hemorrhage / etiology
  • Humans
  • Male
  • Middle Aged
  • Myocardial Infarction / diagnosis
  • Myocardial Infarction / drug therapy*
  • Myocardial Infarction / genetics*
  • Myocardial Infarction / surgery
  • Percutaneous Coronary Intervention
  • Pharmacogenomic Variants*
  • Platelet Activation / drug effects
  • Platelet Aggregation Inhibitors / pharmacology
  • Platelet Aggregation Inhibitors / therapeutic use
  • Platelet Function Tests
  • Polymorphism, Single Nucleotide
  • Prasugrel Hydrochloride / pharmacology
  • Prasugrel Hydrochloride / therapeutic use
  • Purinergic P2Y Receptor Antagonists / pharmacology
  • Purinergic P2Y Receptor Antagonists / therapeutic use
  • Risk Factors
  • Ticlopidine / analogs & derivatives*
  • Ticlopidine / pharmacology
  • Ticlopidine / therapeutic use

Substances

  • Platelet Aggregation Inhibitors
  • Purinergic P2Y Receptor Antagonists
  • Clopidogrel
  • Cytochrome P-450 CYP2C19
  • Prasugrel Hydrochloride
  • Ticlopidine