TABLE 1

Examples of possible endogenous biomarkers of CYP3A activity

Biomarker
11β-HydroxyandrosteroneAcetylarginine
11β-HydroxyetiocholanoloneAllotetrahydrocortisone
11β-HydroxytestosteroneAndrostanolone
11-DehydrocorticosteroneAndrostenedione
11-DeoxycortisolAndrosterone
11β-HydroxyandrostenedioneAndrosterone sulfate
16α-HydroxytestosteroneCholesterol
16α-HydroxyandrostenedioneCortisol
16α-Hydroxy-DHEACortisone
16β-HydroxyestradiolDHEA
17α-Hydroxypregnenoloned-Glucosaminide
24-HydroxycholesterolDHEA sulfate
27-HydroxycholesterolEstradiol
2-HydroxyestradiolEstrone
2-HydroxyestroneEtiocholanolone
4β-HydroxycholesterolGlycochenodeoxycholic acid sulfate
4-HydroxyandrostenedioneHydroxytestosterone sulfate
6β-HydroxyandrostenedioneIndoxyl sulfate
6β-HydroxycortisolMannitol-1-phosphate
6β-Hydroxycortisonep-Cresol sulfate
7α-Hydroxy-DHEAPregnenolone
7β-HydroxycholesterolSaccharopine
7β-Hydroxy-DHEAScyllo-inositol
25-Hydroxyvitamin D3Testosterone
  • These data are from Bodin et al. (2001), Rahmioglu et al. (2011), Wang et al. (2012), Kim et al. (2013), and Shin et al. (2013). Some compounds were identified after PXR induction and have not been verified as being CYP3A substrates or products using standard in vitro methods. DHEA, dehydroepiandrosterone.