Paraoxonase-1 activity affects the clopidogrel response in CYP2C19 loss-of-function carriers

Thromb Res. 2013 Nov;132(5):558-64. doi: 10.1016/j.thromres.2013.09.008. Epub 2013 Sep 13.

Abstract

Background: The impact of paraoxonase-1 (PON1) activity on the response to clopidogrel may differ in patients treated with drug-eluting stents (DES) in association with CYP2C19 loss-of-function (LOF) polymorphisms.

Methods: This study included 112 Japanese patients receiving clopidogrel (75 mg/day) and aspirin (100mg/day) who underwent optical coherence tomography (OCT) examination 9 months after DES implantation. The CYP2C19 genotype was analyzed and LOF carriers (1/2, 1/3, 2/2, 3/3, 2/3) were identified. At the 9-month follow-up, platelet reactivity was determined by measuring the P2Y12 reactivity unit (PRU) using a VerifyNow P2Y12 assay, PON1 activity was evaluated and intra-stent thrombus was evaluated by OCT.

Results: Of the 112 Japanese patients, 75 were LOF carriers (67.0%). The patients were divided into tertiles according to the PON1 activity (tertile 1; <230 U/L, tertile 2; 230-283U/L, tertile 3; >283 U/L). In the VerifyNowP2Y12 analysis, tertile 1 had a higher PRU than tertiles 2 and 3 in LOF carriers, and there was no difference among tertiles in non-carriers. The highest incidence of intra-stent thrombus was observed in tertile 1 followed by tertiles 2 and 3 in LOF carriers, whereas there was no such difference in non-carriers. Multivariate analysis revealed that LOF carriers and PON1 activity tertile 1 were independent predictors of intra-stent thrombus in all patients. In LOF carriers, tertile 1 was the only independent predictor for intra-stent thrombus.

Conclusion: Low PON1 activity is associated with a low response to clopidogrel and a high frequency of intra-stent thrombus only in LOF carriers.

Keywords: CYP; CYP2C19; DES; EES; LOF; MI; OCT; PCI; PES; PON1; PRU; Paraoxonase-1; SES; TLR; VerifyNowP2Y12; clopidogrel; cytochromeP450; drug-eluting stent; everolimus-eluting stent; intra-stent thrombus; loss-of-function; myocardial infarction; optical coherence tomography; paclitaxel-eluting stent; paraoxonase-1; percutaneous coronary intervention; platelet reactivity unit; sirolimus-eluting stent; target lesion revascularization.

Publication types

  • Clinical Trial

MeSH terms

  • Aged
  • Aryl Hydrocarbon Hydroxylases / genetics*
  • Aryldialkylphosphatase / metabolism*
  • Aspirin / therapeutic use*
  • Clopidogrel
  • Cytochrome P-450 CYP2C19
  • Drug-Eluting Stents / adverse effects
  • Female
  • Humans
  • Male
  • Middle Aged
  • Platelet Aggregation Inhibitors / therapeutic use*
  • Polymorphism, Genetic
  • Thrombosis / drug therapy*
  • Thrombosis / enzymology
  • Thrombosis / etiology
  • Thrombosis / genetics
  • Ticlopidine / analogs & derivatives*
  • Ticlopidine / therapeutic use

Substances

  • Platelet Aggregation Inhibitors
  • Clopidogrel
  • Aryl Hydrocarbon Hydroxylases
  • CYP2C19 protein, human
  • Cytochrome P-450 CYP2C19
  • Aryldialkylphosphatase
  • Ticlopidine
  • Aspirin