TABLE 2

CYP3A4 in vitro determined kinetic parameters

Compound
Competitive Inhibition: Ki
Time-Dependent Inhibition
Induction
References by Order of the in Vitro Tool
KI
kinact
 EC50
Emax
μM μM min-1 μM
Atomoxetine 17 Sauer et al., 2004
Atorvastatin 8 Obach et al., 2006
Azithromycin 150 410 0.029 Obach et al., 2006; Venkatakrishnan and Obach, 2007
Carbamazepine 100 55.8 34.3 Fahmi et al., 2008a
Chlorzoxazone 700 Berthou et al., 1995
Cimetidine 115 Obach et al., 2006
Clarithromycin 50 18.9 0.053 Obach et al., 2006; Venkatakrishnan and Obach, 2007
Conivaptan 0.017 8.06 0.073 New Drug Application 021697; unpublished data
Diltiazem 30 1.15 0.027 Obach et al., 2006; Venkatakrishnan and Obach, 2007
Erythromycin 9 13.5 0.041 Obach et al., 2006; Venkatakrishnam and Obach, 2007
Fluconazole 3.4 Obach et al., 2006
Flumazenil 7.5 Unpublished data
Fluoxetine 8 0.606 0.015 0.54 2.1 Obach et al., 2006; Venkatakrishnan and Obach, 2007; Fahmi et al., 2008b
Fluvoxamine 21.5 Galetin et al., 2008
Gatifloxacin 150 Obach et al., 2006
Itraconazole 0.005 Obach et al., 2006
Ketoconazole 0.006 Obach et al., 2006
Mibefradil 0.10 2.3 0.400 4.1 6.5 Prueksaritanont et al.,a 1999; Obach et al., 2006; Fahmi et al., 2008a
Nefazodone 0.45 6.23 0.037 Obach et al., 2007; unpublished data
Nitrendipine 17 18.2 17.4 Unpublished data
Parecoxib 1000 Unpublished data
Ranitidine 150 Obach et al., 2007
Rifampin 100 0.57 33 Fahmi et al., 2008a
Roxithromycin 34 72 0.023 Obach et al., 2007; Polasek and Miners, 2006
Saquinavir 0.41 0.65 0.260 0.9 34.6 Ernest et al., 2005; Obach et al., 2007; Fahmi et al., 2008b
Simvastatin 0.39 25 4 Obach et al., 2007
Terbinafine 150 25 2.3 Obach et al., 2007
Troleandomycin 1.3 2.4 0.032 0.27 15.9 Obach et al., 2007; Fahmi et al., 2008a
Valdecoxib 68 10 2.2 Unpublished data
Verapamil
11.50
0.58
0.07
0.16
16.4
Obach et al., 2007; Venkatakrishnam and Obach, 2007; Fahmi et al., 2008a

  • ↵ a See supplemental data for additional reference information.