TABLE 1

EC50 and Emax values of the inducers for CYP3A4 mRNA and activity in hepatocytes generated from the concentration vs. response curves in Fig. 1

S.D. shown in parentheses.



Inducer

Conc.

mRNA

Activitya

EC50
Emax
n b
R2
EC50
Emax
n
R2
μM μM μM
Donor 1 BST 0.51-50 1.07 (0.48) 11.40 (3.47) 1.3 (0.5) 0.953 0.78 (0.27) 14.75 (0.57) 1.6 (0.8) 0.995
CMZ 1.02-100 20.55 (3.03) 14.30 (0.89) 1.2 (0.1) 0.997 15.30 (0.79) 15.73 (0.57) 2.1 (0.3) 0.994
DEX 1.02-100 50.80 (11.60) 11.10 (1.70) 1.14 (0.2) 0.994 33.8 (5.3) 12.62 (3.43) 1.2 (0.3) 0.992
EFA 0.51-20 1.860 (1.01) 5.80 (0.34) 3.4 (2.6) 0.994 12.50 (3.5) 7.27 (0.77) 1.8 (0.5) 0.987
PB 15.6-1000 155.50 (20.90) 17.90 (1.07) 1.5 (0.2) 0.993 250.00 (92.1) 22.65 (5.57) 0.9 (0.2) 0.985
RIF 0.05-5 0.33 (0.12) 49.70 (5.47) 1.1 (0.4) 0.919 0.25 (0.04) 10.60 (0.60) 1.2 (0.2) 0.987
Donor 2 BST 0.51-50 5.78 (3.88) 17.76 (3.59) 0.8 (0.2) 0.971 1.13 (0.20) 4.63 (0.24) 1.1 (0.2) 0.9889
CMZ 1.02-100 14.37 (4.43) 6.04 (0.79) 1.4 (0.40) 0.976 27.70 (2.72) 4.57 (0.28) 2.6 (0.7) 0.991
DEX 6.25-200 75.20 (14.81) 15.12 (1.48) 0.8 (0.1) 0.960 22.00 (2.40) 5.41 (0.78) 1.2 (0.7) 0.918
EFA 0.51-20 15.74 (5.89) 9.74 (3.08) 0.7 (0.2) 0.986 2.18 (1.40) 3.15 (0.78) 1.2 (0.7) 0.917
PB 15.6-1000 86.19 (7.41) 6.94 (0.25) 1.9 (0.3) 0.992 120.30 (7.9) 8.65 (0.18) 1.4 (0.1) 0.998

RIF
0.01-20
0.22 (0.05)
81.61 (3.54)
1.2 (0.2)
0.981
0.51 (0.08)
12.51 (0.69)
1.2 (0.3)
0.975
  • a CYP3A4 activity (testosterone 6β-hydroxylation) measured in hepatocytes.

  • b Sigmoidity of the curves in Fig. 1.