TABLE 5

Recommended in vitro probe substrates and inactivators for evaluation of TDI (including MBI) of P450 enzymes


Isoform

Substrate

Positive Control TDI

Reference
CYP1A2 Phenacetin Furafylline Kunze and Trager, 1993
Ethoxyresorufin
CYP2B6 Bupropion Ticlopidine Richter et al., 2004
thioTEPA Richter et al., 2005
CYP2C8 Paclitaxel Gemfibrozil-glucuronide Ogilvie et al., 2006
Amodiaquine Phenelzine Polasek et al., 2004
CYP2C9 Diclofenac Tienilic acid Jean et al., 1996
Tolbutamide
S-Warfarin
CYP2C19 S-Mephenytoin Ticlopidine Ha-Duong et al., 2001
Omeprazole
CYP2D6 Dextromethorphan Paroxetine Bertelsen et al., 2003
Bufuralol
CYP3A4 Testosterone Mifepristone He et al., 1999
Midazolam Verapamil Wang et al., 2004
Troleandomycin Atkinson et al., 2005


Erythromycin
McConn, et al., 2004
  • TEPA, N,N′,N″-triethylenethiophosphoramide.