PharmPK Discussion - Correlation of Microsomal assay with invivo metabolism of compounds

• On 22 Jul 2008 at 12:58:09, "Maninder Pal Kaur" (maninder02.aaa.gmail.com) sent the message
  

  
  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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• On 22 Jul 2008 at 20:33:26, Katya.-at-.Apredica.com sent the message
  

  
  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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• On 22 Jul 2008 at 13:15:13, "Maninder Pal Kaur" (maninder02.-a-.gmail.com) sent the message
  

  
  but could it show reverse behaviour like stable in microsomal assay
  but cleared very fast in vivo
  
  

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• On 23 Jul 2008 at 08:42:11, "Tausif Ahmed" (tausif.ahmed.at.ranbaxy.com) sent the message
  

  
  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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