TABLE 3

Details of in vitro P450 inhibition assay conditions and positive control inhibitors

The microsomal protein concentration in each assay was standardized at 0.1 mg/ml.

Substrate[Substrate]Incubation TimePositive Control
μMmin
CYP1A2Phenacetin3510Fluvoxamine furafyllinea
CYP2C8Paclitaxel1010Quercetin phenelzinea
CYP2C9Diclofenac85Sulphaphenazole tienilic acida
CYP2C19S-Mephenytoin5010Ticlopidineb
CYP2D6Bufuralol510Quinidine paroxetinea
CYP3A4Atorvastatin5010Ketoconazole troleandomycina
Midazolam2.55
Nifedipine1010
  • a Positive control for metabolism-dependent inhibition only.

  • b Positive control for reversible and metabolism-dependent inhibition.