TABLE 4

Effect of P450 inhibitors on the metabolism of lonafarnib with human liver microsomes


Inhibitors

Inhibitor Conc.

% of Control Activity Remaininga
M1
M2
M3
M4
Ketoconazole 2 μM 18 27 0 N.D.
α-Naphthoflavone 1.0 μM 103 102 118b 89
Quercetin 20 μM 85 98 70 54
50 μM 96 164c 69 28
CYP3A4/5 monoclonal antibody
2 μg/μg protein
15
25
0
N.D.
  • N.D., not detected, peak below the detection limit.

  • a Activity remaining is calculated as % of vehicle control.

  • b Stimulation by α-naphthoflavone.

  • c Stimulation by quercetin.