TABLE 3

Cocktail incubation approach using pooled HLMs and the Tecan Fluent system

Ten UGT probe substrates were incubated either individually or in cocktails. Values are presented as the mean ± S.D. unless otherwise mentioned.

Cocktail GroupUGT Probe SubstrateUGT IsoformIncubation Concentration Relative Rate (CV)bFold Difference
Individual IncubationCocktail Incubation
µM%
1TrifluoperazineUGT1A45100 ± 3.3111.5 ± 7.31.1
GemfibrozilUGT2B4/2B75100 ± 12.992.1 ± 13.60.9
2AmitriptylineUGT2B105100 ± 10.794.2 ± 20.00.9
OxazepamaUGT2B155100 ± 2.0104.7 ± 21.21.0
3PropofolUGT1A95100 ± 13.3105.1 ± 11.81.1
ZidovudineUGT2B7100100 ± 4.497.5 ± 4.41.0
4Chenodeoxycholic acidUGT1A35100 ± 10.998.0 ± 7.61.0
5-HydroxytryptopholUGT1A65100 ± 12.0101.0 ± 6.11.0
TestosteroneUGT2B175100 ± 3.987.1 ± 7.20.9
5β-EstradiolUGT1A15N/AN/AN/A
  • CV, coefficient of variation; N/A, not applicable.

  • a Incubation of racemic oxazepam.

  • b Data are reported as the relative rate percentage (CV%) (n = 3). The relative rate was measured in the individual incubation and was defined as 100% for each substrate.