CORRESPONDENCE
NATURE MEDICINE VOLUME 17 | NUMBER 9 | SEPTEMBER 2011 1039
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Paraoxonase-1 and clopidogrel efficacy
To the Editor:
We read with great interest the paper published in Nature Medicine
by Bouman et al.
1
showing that a common paraoxonase-1 (PON1)
polymorphism (rs662, also known as Q192R) is a major determinant
of clopidogrel biological efficacy and stent thrombosis, whereas the
common CYP2C19*2 allele (rs4244285-A allele) has no effect in this
population. This suggests that previous data about the effect of the
rs4244285-A allele on clopidogrel efficacy
2,3
were mainly related to
linkage disequilibrium with PON1 polymorphisms.
In an attempt to replicate the results of Bouman et al.
1
, we ana-
lyzed, in an ongoing large French registry, the association between
PON1 rs662 and CYP2C19 rs4244285 polymorphisms and biological
response to clopidogrel in 482 individuals with unstable coronary
artery disease in Marseille. Subject characteristics are included in
Supplementary Table 1. All patients were treated with 600 mg clopi-
dogrel followed by clopidogrel 150 mg maintenance therapy. Platelet
reactivity was assessed using 10 mM ADP (reported as ADP–induced
platelet aggregation (ADP-Ag) values), and the specific pharmaco-
logical response to clopidogrel was assessed by detecting phospho-
rylation of vasodilator-stimulated phosphoprotein (VASP; reported
as platelet reactivity index VASP (PRI VASP) values) between 12 and
24 h after hospital discharge and at 30 d after hospital discharge.
CYP2C19 rs4244285 and PON1 rs662 genotyping was performed
using amplification refractory mutation system PCR. PON1 rs662
genotyping was checked with restriction fragment length polymor-
phism PCR and Sanger sequencing. All methods are detailed in the
Supplementary Methods. The study protocol was approved by the
University Hospital La Timone Ethics Committee, and patients gave
written informed consent for their participation.
Platelet reactivity and clopidogrel response were not affected by
PON1 rs662 polymorphism status, either when measured shortly after
the loading dose or after steady-state maintenance therapy (Fig. 1
and Supplementary Tables 2 and 3). Conversely, a strong influence
of the CYP2C19 rs4244285 genotype on both platelet reactivity and
clopidogrel response was observed at both time points (Fig. 1 and
Supplementary Tables 2 and 3), as previously reported by our group
and others
2,3
.
The lack of PON1 rs662 genotype influence on clopidogrel effi-
cacy observed in our cohort may have several potential explanations.
First, the present study might be underpowered to find a PON1 rs662
polymorphism effect; however, Bouman et al.
1
described a significant
effect on clopidogrel response with a smaller sample size. Second,
the selected unstable patients and high clopidogrel doses used in
our study might have affected our results compared with standard
clopidogrel doses for stable patients in the Bouman et al.
1
study.
Moreover, the choice of platelet tests and timing of platelet testing
was different, as this was done 12 to 24 h after loading dose and 30 d
after the onset of acute coronary syndrome in our study. Bouman et
al.
1
tested clopidogrel pharmacological response using 20 mM ADP
or active metabolite. Here we used 10 mM ADP and also used the
most specific pharmacological test available to assess clopidogrel
response, the PRI VASP assay. Finally, confounding factors may have
influenced our results, as PON1’s enzymatic activity is affected by
several environmental factors including chronic renal disease, lipids,
smoking and inflammation. Indeed, the individuals in our study were
in a Mediterranean city, which might be slightly different from the
population studied by Bouman et al.
1
. However, the baseline charac-
teristics of the patients according to PON1 rs662 polymorphism were
not different between genotypes in our cohort (data not shown). On
the basis of our results, the necessity for PON1 rs662 genotyping in
routine clinical practice seems questionable. Further large studies are
urgently needed to address the observed discordance between our
study and that of Bouman et al.
1
and the potential relevance of PON1
genotyping to tailor antiplatelet therapy.
Note: Supplementary information is available on the Nature Medicine website.
ACKNOWLEDGMENTS
We thank N. Saut for her technical assistance.
COMPETING FINANCIAL INTERESTS
The authors declare no competing financial interests.
Thomas Cuisset
1,2
, Pierre-Emmanuel Morange
2
, Jacques Quilici
1
,
Jean Louis Bonnet
1
, Christian Gachet
3
& Marie-Christine Alessi
2
1
Département de Cardiologie, University Hospital La Timone, Marseille,
France.
2
Institut National de la Santé et de la Recherche Médicale, U626,
Faculté de Médecine, Marseille, France.
3
UMR-S949 Institut National de la
Santé et de la Recherche Médicale-Université de Strasbourg, Etablissement
Français du Sang-Alsace, Strasbourg, France.
1. Bouman, H.J. et al. Nat. Med. 17, 110–116 (2011).
2. Mega, J.L. et al. N. Engl. J. Med. 360, 354–362 (2009).
3. Frere, C. et al. Am. J. Cardiol. 101, 1088–1093 (2008).
30
40
50
60
70
80
30
40
50
60
70
80
P = 0.20 P = 0.22
PON1 rs662
ADP- Ag (%)
AA AG GG AA AG GG
30
40
50
60
70
80
P = 0.11 P = 0.05
PON1 rs662
PRI VASP (%)
30
40
50
60
70
80
P = 0.007 P < 0.0001
CYP2C19 rs4244285
ADP- Ag (%)
P = 0.002 P < 0.0001
PRI VASP (%)
Assessment after 600 mg loading dose Assessment on 150 mg maintenance therapy
CYP2C19 rs4244285
AA AG GG AA AG GG AA AG GG AA AG GG
AA AG GG AA AG GG
Figure 1 Platelet parameters according to PON1 rs662 and CYP2C19
rs4244285 genotypes. Platelet reactivity was assessed using the 10 mM
ADP-Ag assay and the specific pharmacological response to clopidogrel by
the PRI VASP assay.
© 2011 Nature America, Inc. All rights reserved.