Besides CYP2C19*2, the variant allele CYP2C9*3 is associated with higher on-clopidogrel platelet reactivity in patients on dual antiplatelet therapy undergoing elective coronary stent implantation

Ankie Harmsze, Jochem W van Werkum, Heleen J Bouman, Henk J Ruven, Nicolien J Breet, Jurrien M Ten Berg, Christian M Hackeng, Mathieu M Tjoeng, Olaf H Klungel, Anthonius de Boer, Vera H Deneer

Research output: Contribution to journalArticleAcademicpeer-review

Abstract

INTRODUCTION: The prodrug, clopidogrel, plays an important role in the prevention of thrombotic events in patients undergoing coronary stenting. However, a substantial number of atherothrombotic events still occur, which can partially be explained by heightened residual platelet reactivity. Several studies report that the genetic variation in CYP2C19 (*2) is associated with an impaired response to clopidogrel.

OBJECTIVES: To evaluate the effect of genetic variants affecting clopidogrel's absorption (ABCB1 C1236T, G2677T/A, C3435T), metabolism (CYP2C9*2, *3, CYP2C19*3, CYP3A4*1B, and CYP3A5*3), and pharmacodynamics (P2Y1 A1622G) on top of the influence of CYP2C19*2 on platelet reactivity in patients undergoing elective coronary stenting on dual antiplatelet therapy.

METHODS: Platelet function was assessed by light transmittance aggregometry and VerifyNow P2Y12 assay in 428 consecutive patients. Patients were either on chronic clopidogrel maintenance therapy (75 mg/day for > or =5 days before the intervention) or received a 300 mg clopidogrel loading dose (1-5 days before the intervention, followed by 75 mg/day). Linear and logistic regressions were used to assess the associations between genetic variants and platelet reactivity and poor responder status.

RESULTS: In both the treatment groups, CYP2C19*2-carriage was associated with higher platelet reactivity (P<0.002) and poor responder status; 75 mg group: adjusted odds ratio (ORadj): 3.8, 95% confidence interval (CI): 2.0-7.2, 300 mg group: ORadj: 4.1, 95% CI: 1.6-10.4. In the 300 mg group, CYP2C9*3-carriage was associated with higher platelet reactivity (P<0.05) and poor responder status (ORadj: 11.1, 95% CI: 1.6-78.8, P=0.016).

CONCLUSION: Besides CYP2C19*2, the variant allele CYP2C9*3 plays an important role in the response to clopidogrel in patients on dual antiplatelet therapy undergoing coronary stenting.

Original languageEnglish
Pages (from-to)18-25
Number of pages8
JournalPharmacogenetics and Genomics
Volume20
Issue number1
DOIs
Publication statusPublished - Jan 2010

Keywords

  • Alleles
  • Aryl Hydrocarbon Hydroxylases
  • Blood Platelets
  • Coronary Disease
  • Cytochrome P-450 CYP2C19
  • Cytochrome P-450 CYP2C9
  • Dose-Response Relationship, Drug
  • Female
  • Genetic Variation
  • Genotype
  • Haplotypes
  • Humans
  • Male
  • Middle Aged
  • Platelet Aggregation Inhibitors
  • Platelet Function Tests
  • Prospective Studies
  • Stents
  • Ticlopidine

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