Table 1

Competitive inhibitors of human microsomal midazolam 1′-hydroxylase (CYP3A4)

InhibitorKi(apparent)
μM
LY3038701.8  ± 0.2
LY3509652.2  ± 0.3
LY3359793.8  ± 0.8
Terfenadine4.7  ± 0.7
LY2138296.6  ± 0.9
Nifedipine1-a 22.1  ± 2.4
LY33437043.05  ± 3.7
Omeprazole43.6  ± 5.7
LY3076401-b 59.4  ± 6.0
Erythromycin1-a 194.1  ± 22.9
Cimetidine1-a 267.7  ± 20.4
LY2773591-c 297.7  ± 55.6
LY237216492.7  ± 72.3
LY024410701.3  ± 106.3

The inhibitor constant was determined as described in the text. Parameter estimate ± S.E. of the parameter estimate.

  • ↵1-a Wrighton and Ring (1994).

  • ↵1-b VandenBranden et al. (1996).

  • ↵1-c Ring et al. (1994).