Assessment of cytochrome P450 induction in human hepatocytes using the cocktail strategy plus liquid chromatography tandem mass spectrometry.

A fast and sensitive method was developed for the assessment of CYP induction in human hepatocytes cultured in 96-well plates. The effects on CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, and CYP3A4 were examined by means of mass spectrometry and the well-known cocktail strategy. The performance of the method was tested by using prototypic inducers such as methylcolanthrene, phenobarbital and rifampicin.

A new in vitro approach for the simultaneous determination of phase I and phase II enzymatic activities of human hepatocyte preparations.

Primary hepatocytes are still the best qualified in vitro system to anticipate drug metabolism in man. Recent advances in hepatocytes cryopreservation have notably increased their use not only for drug metabolism studies, but also for other applications such as cell transplantation. Evaluation of the drug-metabolizing competence of each hepatocytes preparation is needed.