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The following message was posted to: PharmPK
Hi All,
To verify the interaction of our products with substrates of CYP2C19, we
use Mephenytoin and quantify (MRM mode) its oxidized metabolite.
But its rate of metabolisation is low on microsomes (less than 0.5%) and
it's sometimes difficult to be enough sensitive.
Does anyone use Mephenytoin as substrate ?
Does anyone use another specific substrate of the 2C19 ?
We would like to use Omeprazole but its oxidized metabolite is non
avalaible.
Thank you for your help.
Regards,
Fabrice Guillet
Bioanalytical Group
Fournier Pharma
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The following message was posted to: PharmPK
Dear all,
To verify the interaction of our products with substrates of CYP2C19, we
use Mephenytoin and quantify (MRM mode) its oxidized metabolite.
But its rate of metabolisation is low on microsomes (less than 0.5%) and
it's sometimes difficult to be enough sensitive.
Does anyone use Mephenytoin as substrate for this kind of test?
Does anyone use another specific substrate of the 2C19 ?
We would like to use Omeprazole but its oxidized metabolite is non
available.
Thank you for your help.
Regards,
Fabrice Guillet
Bioanalytical Group
Fournier Pharma
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Dear David,
For the same purpose, we used S-mephenytoin as the substrate in the
CYP2C19 Inhibition assay without success due to insufficient
sensitivity by LC-MS/MS detection of the metabolite.
Then we used omeprazole as the substrate and validated this assay.
This assay now works well in our lab and we routinely offer this
assay to our customers. You were right, the metabolite, 5-hydroxy
omeprazole, was not commercially available when we were looking for
it. We then managed to purchase it through a customer-synthesis from
SynFine, a Canadian company at http://www.synfine.ca/
I hope that this information is helpful and good luck with your
research. Please feel free to contact me should you become
interested in our services.
Best regards,
Cheryl
--
X. Cheryl Wu, Ph.D.
Director of Pharmaceutical Sciences
Cerep, Inc.
15318 NE 95th Street
Redmond, WA 98052, USA
Tel: 1-425-895-8666 x226
Fax: 1-425-895-8668
Mail to: c.wu.-a-.cerep.com
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