Cytochrome P450 Inhibition

Because of the important role of Cytochrome p450 enzymes in drug metabolism, it is important to assess the ability of lead compounds to inhibit specific cytochrome p450 enzymes to avoid potential drug-drug interactions where one drug may affect the metabolism of another. This assay is only recommended for advanced leads.

Typical Assay Conditions

IsoformSourceSubstratePositive Inhibitor
1A2 BD Bioscience Supersome phenacetin furfylline
2C9 BD Bioscience Supersome diclofenac sulfaphazole
2C19 BD Bioscience Supersome mephenytoin ticlopidine
2D6 BD Bioscience Supersome bufuralol quinidine
3A4 BD Bioscience Supersome Under-redevelopment ketaconazole

Assay Format: 9 point curve for IC50 determination
Analysis: LC-MS/MS of specific drug probe metabolite
Requirements: 150 microliters of 10 mM drug stock