Table 2

mAb3A4a-mediated inhibition of the metabolism of marker substrates by human liver microsomes

SubstrateConcentration2-a% Control2-b (+ mAb)SubstrateConcentration% Control (+ mAb)
μM μM
Testosterone2501.97  ± 0.05Bufuralol50115.2  ± 0.23
(CYP3A4)2-c 752.60  ± 0.00(CYP2D6)15111.9  ± 9.08
254.55  ± 0.065106.8  ± 14.5
Chlorzoxazone500104.7  ± 6.37Diclofenac100108.3  ± 1.16
(CYP2E1)100103.6  ± 0.56(CYP2C9)30113.1  ± 1.14
20119.8  ± 0.310125.7  ± 0.15
(S)-Mephenytoin40099.5  ± 1.41Phenacetin1000101.9  ± 1.75
(CYP2C19)12094.6  ± 4.33(CYP1A2)150107.5  ± 1.12
4096.4  ± 1.9925113.9  ± 0.91
  • 2-a Concentration of substrate used for metabolism.

  • 2-b Percentage of control was determined as the difference of activity values between the presence and absence of mAb3A4a.

  • 2-c Individual P-450 activities were probed with respective marker substrates.