Table 1

The in vitro rates of formation (picomoles per minute per milligram of microsomal protein) of metabolites by characterized human hepatic microsomes in incubations with 25 or 100 μM NVP

Microsomes1-aNVP Metabolite
2-HydroxyNVP3-HydroxyNVP8-HydroxyNVP12-HydroxyNVP
25 μM100 μM25 μM100 μM25 μM100 μM25 μM100 μM
22.9916.230.462.740.091.791.719.24
30.322.010.131.09ND0.220.371.62
50.171.950.300.74ND0.240.381.78
64.1522.662.507.090.453.062.7113.59
70.663.880.111.34ND0.530.863.61
90.692.991.122.790.220.650.562.23
100.471.33ND0.35ND0.170.441.73
112.7810.603.699.030.432.751.937.61
120.921.690.160.77ND0.250.331.45
131.575.370.450.980.140.590.903.46
Mean ± S.D.1-b 1.47 ± 1.376.87 ± 7.320.99 ± 1.272.69 ± 2.980.26 ± 0.171.03 ± 1.101.02 ± 0.824.63 ± 4.14
  • ND = Not detected

  • 1-a Microsome identification number provided by Human Biologics, Inc. (Phoenix, AZ).

  • 1-b n = 10, except for 3-hydroxyNVP (25 μM) where n = 9 and 8-hydroxyNVP (25 μM) wheren = 5.