Inhibitor (Concentration) | Percentage Inhibitiona | ||||||
---|---|---|---|---|---|---|---|
M10 | M11 | M14 | M15 | ||||
Antibody (1×, CYP2C8)b | 18.2 | —c | — | 75.9 | |||
Montelukast (3 μM, CYP2C8)b | 17.0 | — | — | 78.5 | |||
Sulfaphenazole (20 μM, CYP2C9)d | 29.4 | 42.9 | 33.3 | — | |||
Tranylcypromine (30 μM, CYP2C19)d | 38.2 | 71.4 | 58.3 | 40.9 | |||
Quinidine (15 μM, CYP2D6)d | 5.9 | 57.1 | 41.7 | 4.5 | |||
Ketoconazole (10 μM, CYP3A4)d | 38.2 | 57.1 | 91.7 | 59.1 | |||
1-Aminobenzotriazole (1 mM, All P450s)d | 70.6 | 71.4 | 91.8 | 86.4 |
↵ a Percentage Inhibition = (amount of the metabolite in the absence of inhibitor — amount of the metabolite in the presence of inhibitor)/(amount of the metabolite in the absence of inhibitor).
↵ b Human liver microsome B was used and muraglitazar concentration was 25 μM.
↵ c —, no inhibition observed.
↵ d Human liver microsome A was used and muraglitazar concentration was 26.6 μM.