Cytochromes P450 (CYP) are the main enzymes involved in drug metabolism. They may be induced by exogenous substances, causing drug interactions.

If a cytochrome P450 is induced by a compound, it can increase the metabolism of a co-administered drug which is the substrate of the induced enzyme.

The consequence of induction is a reduction in systemic exposure and therefore in the efficacy of a co-administered treatment or of the medicinal product itself.

This test identifies the potential of test compounds to induce CYP1A2, CYP2B6 or CYP3A4, using cryopreserved human hepatocytes.

Protocol

MatrixHuman cryopreserved plateable hepatocytes 
CofactorNADPH
Test concentrations1, 10 et 30 µM
Treatment duration2x 24 heures
Controls

Omeprazol (1A2), carbamazepine (2B6), rifampicin (3A4)

Analysis methodLCMS-MS
Data deliveryInduction factor with respect to the vehicle

 

Data

Note

It is recommended to do the study with 3 individual donors