TABLE 2

Competitive inhibition constant, Ki, estimated from 3- and 10-min incubation in rCYP3A (+b5) and HLMs using competitive inhibition model

Data are presented as mean ± S.D.



rCYP3A4 (+b5)

HLMs

3 min
10 min
3 min
10 min
ERY 55 ± 13 14.3 ± 4 73 ± 18 29 ± 19.8
nd-ERY 67 ± 11 8.2 ± 2.3 77 ± 12 19.8 ± 12.2
DTZ 5.9 ± 2.1 2.8 ± 0.5 41 ± 9 5.1 ± 3.1
nd-DTZ
0.6 ± 0.09
0.09 ± 0.2
0.8 ± 0.1
0.6 ± 0.24