CYP Induction

The induction of CYP isoenzymes is one of the key aspects in drug-drug interaction.
The induction of CYP isoenzymes by test item is investigated using plated cryopreserved or freshly isolated human primary hepatocytes. The relative fold induction compared to the solvent control is calculated on the level of mRNA, protein and/or enzymatic activity and compared with that of known reference inducers.

Quantity of test item required: 10 mg
Turnaround time of draft report: 10-40 working days

Study Design

• cytotoxicity pre-test (optional)
• triplicates
• 48 h recovery phase
• 24 to 72 h induction phase
• one concentration of primary hepatocytes (freshly isolated or cryopreserved)
• one to three concentrations of test item
• negative control: solvent control
• positive control: CYP reference inducers:

1A2 (omeprazole)
2A6 (pyrazole)
2B6 (phenobarbital, rifampicin)
2C9 (phenobarbital)
2C19 (phenobarbital, rifampicin)
2E1 (ethanol)
3A4 (rifampicin)

Analytics

• enzymatic acitivity (CYP marker reactions)
• mRNA level (real time PCR)
• CYP protein content (Western blotting)

Please inquire for further phase I and II enzyme marker reactions and reference inducers.

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