TABLE 2

In vitro inhibition of hepatic CYP1A2, CYP2C9, CYP2D6, and CYP3A4 in 8HUM and HLM microsomal fractions

Data are presented as percent of activity measured in the absence of inhibitor. Values are mean ± S.D. from a minimum of 3 determinations. Other experimental details are given in Materials and Methods.

InhibitorsCaffeine (Paraxanthine)Debrisoquine (4-OH Debrisoquine)Tolbutamide (OH-Tolbutamide)Midazolam (1-OH-Midazolam)
HLM8HUMHLM8HUMHLM8HUMHLM8HUM
Furafylline (CYP1A2)53 ± 6*56 ± 13*65 ± 991 ± 13103 ± 2563 ± 1995 ± 892 ± 7
Enoxacin (CYP1A2)58 ± 15*52 ± 8*82 ± 2989 ± 1372 ± 2773 ± 1399 ± 1390 ± 4
Fluconazole (CYP2C9/CYP3A4)114 ± 37100 ± 3196 ± 988 ± 1935 ± 21*41 ± 33*29 ± 4***42 ± 5***
Sulfaphenazole (CYP2C9)78 ± 2667 ± 1579 ± 2588 ± 3614 ± 4**28 ± 15**107 ± 21125 ± 41
Quinidine (CYP2D6)105 ± 2874 ± 722 ± 5*43 ± 5*75 ± 17132 ± 2983 ± 997 ± 18
Paroxetine (CYP2D6)66 ± 2695 ± 2252 ± 11*13 ± 5**113 ± 50117 ± 3491 ± 8109 ± 17
Ketoconazole (CYP3A4)135 ± 4585 ± 34142 ± 42152 ± 11154 ± 6692 ± 116 ± 2***11 ± 2***
  • * P < 0.05, **P < 0.01, ***P < 0.001, compared with no inhibitor; unpaired t test, two-tailed P values;