CYP INDUCTION

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Toxicity due to increase activity and decreased exposure of co administered drugs are the clinical effects of CYP induction. 

The potential of compounds inducing CYP1A2, CYP2B6 or CYP3A4 mRNA and/or activity levels in cultured human hepatocytes can be evaluated.

CYP Induction Assay Protocol:

Test article concentration: 5  µM or Cmax (other upon request) 

Incubation time: 3 days 

Incubation temperature: 37 C 

Number of Replicates: n = 2  

Assay condition: Hepatocytes

Assay matrix: CYP1A2, CYP2B6, and CYP3A4 

Controls: Omeprazole (CYP1A2); Phenobarbital (CYP2B6); Rifampicin (CYP3A4) 

Substrates: Phenacetin (CYP1A2); Bupropion (CYP2B6); Midazolam (CYP3A4) 

Analysis Method: qPCR; LC/MS/MS 

Data Delivery: Fold induction (mRNA); Metabolite concentration