TABLE 5

FG and maximum FG ratio values for nine CYP3A4 substrates


CYP3A Substrate

FG

Maximum FG′/FGa

Reference
Buspirone 0.21 4.76 Obach et al. (2006)
Cyclosporine 0.39 2.6 Hebert et al. (1992)
Felodipine 0.45 2.2 Lundahl et al. (1997)
Midazolam 0.57 1.75 Thummel et al. (1996)
Triazolam 0.6 1.67 Masica et al. (2004)
Simvastatin 0.66 1.51 Obach et al. (2006)
Nifedipine 0.74 1.35 Holtbecker et al. (1996)
Quinidine 0.9 1.11 Damkier et al. (1999)
Alprazolam
0.98
1.02
Hirota et al. (2001)
  • a Complete intestinal inhibition is assumed (FG′ = 1).