TABLE 1

Inhibition of CYP2C8 activities by montelukast


Activity

System

Microsomal Protein Concentration

Ki (Mean ± S.E.)
mg/ml μM
Amodiaquine N-deethylase Pooled human liver microsomes 0.025 0.014 ± 0.001
HG42 (high CYP2C8 activitya) 0.025 0.018 ± 0.001
HG43 (low CYP2C8 activityb) 0.025 0.038 ± 0.004
rhCYP2C8 0.005 0.0092 ± 0.0009
Rosiglitazone N-demethylase Pooled human liver microsomes 0.05 0.11 ± 0.02
rhCYP2C8 0.025 0.019 ± 0.002
Paclitaxel 6α-hydroxylase
Pooled human liver microsomes
0.25
0.15 ± 0.02
  • a 480 pmol/mg · min CYP2C8 paclitaxel 6α-hydroxylase activity.

  • b 60 pmol/mg · min CYP2C8 paclitaxel 6α-hydroxylase activity.