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Hi
Can we corrrelate in vitro microsomal assay data to in vivo metabolism
of compounds, to be more precise : is it possible to shortlist
compounds on the basis of microsomal assay and make an assumption that
compounds which are stable in microsomal assa would be more stable
metabolically in vivo as well.
Thanks
Maninder
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The following message was posted to: PharmPK
Maninder, yes, but you need to remember that:
1) All metabolism is species-specific
2) You are looking at this particular organ metabolism only (there
could be plasma or kidney metabolism going on, e.g.)
3) The phase I and II metabolism information may be obtained with
microsomes as well with addition of appropriate cofactors
4) This is ranking and comparison data, not the absolute certainty.
Katya Tsaioun
Apredica
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but could it show reverse behaviour like stable in microsomal assay
but cleared very fast in vivo
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The following message was posted to: PharmPK
Dear Maninder,
In vitro microsomal assays are only used for screening or rank ordering
the compounds. They may or not correlate with the inv vivo situation.
Ultimately the fate of the compound may be decided by its in vivo
efficacy. It may be possible that the compound is highly unstable in
vitro but is very potent due the formation of metabolites. So there is
no general rule on this.
Regards
Dr. Tausif Ahmed
Metabolism and PK
Ranbaxy Research Laboratories
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