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Calendar of Events

Date Event Name
May 26 - 28, 2013 DDI Marbach Castle Conference

Ex Vivo Enzyme Induction

 

Studies of ex vivo induction in the rat, mouse, dog or monkey can provide valuable information to the investigation of a drug candidate.  Not only are these types of induction studies cost-effective, they can provide the following information to your investigation:

  • Which prototypical CYP inducers the drug candidate resembles 
  • Epigenetic tumor formation 
  • Which species most closely resembles human  
  • Drug-drug interactions
  • Pharmacokinetic tolerance
  • Increased elimination (auto-induction)

Assay Selection

CYP1A      7-Ethoxyresorufin O-dealkylation
CYP2A6    Coumarin 7-hydroxylation
CYP2B      Resorufin O-dealkylation
CYP2B      Testosterone oxidation
CYP2C      Testosterone oxidation
CYP2D6    Dextromethorphan O-demethylation
CYP2E1    Chlorzoxazone 6-hydroxylation
CYP2E1    4-Nitrophenol hydroxylation
CYP3A      Testosterone oxidation
CYP4A      Lauric acid hydroxylation
Western blot analysis

Test System

Microsomes prepared from treated tissue.

Automation and Analysis

Tecan liquid-handling system
Validated LC/MS/MS methods
High-throughput Shimadzu autosamplers
Deuterated internal standards

Inducers

β-naphthoflavone
phenobarbital
isoniazid
dexamethasone
rifampin
clofibric acid