TABLE 8

Comparison of incubation conditions along with IC50 values (and the fold shift) with and without NADPH (curves B and C) for the dilution methods

All IC50 values are based on the final or postdilution concentrations.

P450 EnzymeSubstrate/InhibitorThis StudyPerloff et al., 2009 aObach et al., 2007 a
[HLM]TimeFold DilutionIC50Fold Shift (B/C)[HLM]TimeFold DilutionIC50Fold Shift (B/C)a[HLM]TimeFold DilutionIC50Fold Shift (B/C)a
BCBCBC
mg · ml1minμMmg · ml1minμMmg · ml1minμM
CYP1A2Phenacetin/furafylline0.15103.40.036940.210108.40.0214000.0330101.50.02756
CYP2B6Bupropion/ticlopidine0.15100.200.0395.10.15100.840.048180.0520100.130.0314.2
CYP2C8Amodiaquine/gemfibrozil glucuronide0.0125510270.28960.02510260.46570.0251010N.D.N.D.N.D.
CYP2C9Diclofenac/tienilic acid0.15100.920.057160.055101.70.049350.0310100.430.02716
CYP2C19S-Mephenytoin/S-fluoxetine0.1510611.4440.3105853.1270.24010N.D.N.D.N.D.
CYP2D6Dextromethorphan/Paroxetine0.15101.50.053280.15101.10.066170.0310100.230.01219
CYP3A4Midazolam/azamulin0.055100.340.031110.025100.150.0025600.03410N.D.N.D.N.D.
Midazolam/diltiazem0.05510781.2650.025101003.4290.03410543.715
Midazolam/verapamil0.05510250.41610.02510250.34730.03410120.12100
CYP3A4Testosterone/azamulin0.15100.460.044100.0510100.0980.0077130.031010N.D.N.D.N.D.
Testosterone/diltiazem0.15101382.2630.0510101302.8460.031010551.831
Testosterone/verapamil0.1510290.38760.051010280.271040.0310108.20.1555
  • N.D., no data.

  • a Calculated based on published values.