CB, maximum daily dose, and Cmax of the tested compounds

Test compounds (10 μM) were incubated with human liver microsomes in the presence of NADPH (first arm), NADPH and UDPGA (second arm), or NADPH, UDPGA, and GSH (third arm) or with hepatocytes (fourth arm). The CB amounts were determined with duplicate incubations. Daily dose and Cmax represent the maximum daily dose and the maximum concentration at the maximum daily dose, respectively. Daily dose and Cmax are from the package inserts or the following references: 1) Maass et al., 1982; 2) Durand et al., 1992; 3) Boni et al., 1997; 4) Greene and Barbhaiya, 1997; 5) Fontana et al., 1998; 6) Kalgutkar and Soglia, 2005; 7) Walgren et al., 2005; and 8) Lammert et al., 2008.

Daily DoseCmaxReference
pmol/mg proteinmg/dayng/ml
Positive compounds
    Acetaminophen1791242816400082,400a6, 7
    Alpidem4401928810115065.7a2, 6, 7
    Bromfenac5110744221009240a3, 6, 7, 8
    Carbamazepine11990351812009000a6, 7
    Diclofenac12017359492003320a6, 7, 8
    Flutamide4774712253575078.0a6, 7
    Nefazodone13649973062546002760a4, 6, 7, 8
    Tacrine264201471420078.5a5, 6, 7, 8
    Ticlopidine128611362496050019506, 7
    Tienilic acid5384871242850057,0001, 6, 7, 8
    Troglitazone117096727311860028206, 7
Negative compounds
    Acetylsalicylic acidN.D.N.D.N.D.33001840
  • N.D., CB for test compounds was lower than that for the control without NADPH and UDPGA.

  • a Cmax value normalized by dose.

  • b Cmax value normalized by body weight.