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Dear all,
Please find below the list of NCE behavior in different assays
1. Highly unstable with rat liver microsomes, but stable in
case of dog and Human liver microsomes
2. PK in rats: IV pk is fairly good, but oral bioavailability
is <10%
3. Preliminary Efficacy in rats: Good efficacy
* We are in process of doing metabolic stability using intestinal
microsomes and to find out the invitro potency of some of identified
metabolites.
* But we believe that compound itself showed in vivo activity but
not the metabolite
Question: Could you please comment on this NCE.
Whether it is good or bad, whether we can do further studies.
Thanks in advance,
Samiulla
Aurigene
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The following message was posted to: PharmPK
Just out of curiosity, was the dosing for the efficacy study oral or IV?
-Rachel
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The following message was posted to: PharmPK
Hi,
I would like to check metabolite stability in rat, dog
monkey, and human hepatocytes. In addition, I would
also like to check bioavailability in dog and monkey.
Xiaodong
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Dear Dr Samiulla
From the data you have provided your drug would seem an ideal
candidate for a human microdose study. Please see www.xceleron.com
Professor Colin Garner
CEO, Xceleron
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Its oral route.
Samiulla
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