TABLE 4

Lack of time-dependent CYP3A inactivation by MD


MD

HLM Protein Bindinga (Percentage Free)

Percentage of MD Remainingb

Percentage of CYP3A Activitiesb
0.4 μM 88 (5) N.D. N.D.
1 μM N.D. 109 (7) 96 (5)
2 μM N.D. 101 (6) 103 (9)
4 μM
83 (5)
111 (13)
106 (5)
  • N.D., not determined.

  • a Calculated according to eq.1. Values are mean (S.D.), n = 4 incubations at 0.2 mg/ml HLMs.

  • b Calculated as the percentage remaining at 12 min tested in the inactivation experiments. Values are mean (S.D.), n = 3 incubations.