TABLE 4

DME activities of cryopreserved human enterocytes from 24 donors

The mathematical average (mean) and S.D. of the 24 donors are calculated from the results of each individual donor. The DME pathways evaluated were as follows: CYP2C9 (diclofenac 4-hydroxylation), CYP2C19 (S-mephenytoin 4-hydroxylation), CYP3A4 [midazolam 1′-hydroxylation (CYP3A4M) and testosterone 6β-hydroxylation (CYP3A4T)], CYP2J2 (astemizole O-demethylation), CES (irinotecan hydrolysis), UGT (7-hydroxycoumarin glucuronidation), and SULT (7-hydroxycoumarin sulfation) activities. Mean and S.D. values of the activities of the 24 donors are shown at the bottom of the table.

Lot NumberActivity (pmol/min/million Enterocytes)
CYP2C9CYP2C19CYP3A4MCYP3A4TCYP2J2CES2UGTSULT
HE30051.680.562.67ND1.20.238.388.72
HE30060.590.290.136.230.730.332.32.04
HE30070.910.390.9922.70.570.463.084.04
HE30080.460.680.87NA0.330.551.81.79
HE30091.180.350.7232.10.250.64.327.78
HE30101.210.620.4617.50.990.412.563.32
HE30110.030.010.092.60.330.291.011.7
HE30140.440.110.48.21.180.173.552.66
HE30152.50.492.55ND0.950.517.335.23
HE30162.051.080.9926.70.930.345.714.13
HE30190.240.110.35.270.260.31.471.89
HE30200.310.140.4912.90.580.595.831.84
HE30210.20.060.172.970.190.081.491.64
HE30272.020.310.6825.90.760.193.682.69
HE30280.680.210.82260.710.33.849.02
HE30290.860.120.5912.10.760.086.553.65
HE30300.260.280.2914.90.320.05158.3
HE30310.340.090.162.950.490.181.60.79
HE30321.840.811.343.40.820.245.94.5
HE30332.111.131.0328.40.70.1129.614.2
HE30347.930.714.3545.21.980.12122.68.24
HE30400.960.781.0032.300.300.1823.8022.00
HE30420.230.031.6631.201.060.0674.208.98
HE30431.390.210.6218.800.550.239.139.00
Mean1.270.400.9719.920.710.2814.365.76
S.D.1.590.330.9912.990.410.1727.744.88
  • NA, not applicable; ND, not determined.