TABLE 3

DME activities of cryopreserved human enterocytes

Enterocytes from 4 male (HE3005, HE3007, HE3008, HE3010) and 4 females (HE3006, HE3009, HE3011, HE3013) were pooled and used in the study. The DME pathways evaluated were as follows: CYP1A2 (phenacetin hydroxylation), CYP2A6 (coumarin 7-hydroxylation), CYP2B6 (bupropion hydroxylation), CYP2C8 (paclitaxel 6α-hydroxylation), CYP2C9 (diclofenac 4-hydroxylation), CYP2C19 (S-mephenytoin 4-hydroxylation), CYP2D6 (dextromethorphan hydroxylation), CYP2E1 (chlorzoxazone 6-hydroxylation), CYP3A4 [midazolam 1′-hydroxylation (CYP3A4M) and testosterone 6β-hydroxylation (CYP3A4T)], CYP2J2 (astemizole O-demethylation), UGT (7-hydroxycoumarin glucuronidation), SULT (7-hydroxycoumarin sulfation), and CES2 (irinotecan hydrolysis) activities. Results are mean and S.D. of triplicate determinations. Activities for CYP1A2, CYP2A6, CYP2B6, and CYP2D6 were below quantifiable levels (BQL).

DME PathwaySpecific Activity (pmol/min/million Enterocytes)
MeanS.D.
CYP1A2BQLNA
CYP2A6BQLNA
CYP2B6BQLNA
CYP2C80.20
CYP2C92.00.2
CYP2C190.40.1
CYP2D6BQLNA
CYP2E10.40.1
CYP3A4M2.80.5
CYP3A4T19.25.8
CYP2J21.60.1
CES20.30
UGT4.50.3
SULT11.40.7
  • NA, not applicable.