Drug | Classification | CYP3A4/5 | CYP2C9 | CYP1A2 | CYP2D6 |
---|---|---|---|---|---|
Flutamide | Antiandrogen | 98 | — | — | — |
Rosiglitazone | Antidiabetic | 37 | — | 71 | 31 |
Metformin hydrochloride | Antidiabetic | 63 | 23 | 32 | 63 |
Coenzyme B12 | Vitamin | 56 | — | — | — |
Pyrvinium pamoate | Anthelmintic | 54 | — | — | — |
Diclofenac sodium | Anti-inflammatory | — | 54 | — | — |
Avocatin B | Antibacterial, antifungal | 52 | — | — | — |
Nilutamide | Antiandrogen | 49 | — | — | — |
Deracoxib | Anti-inflammatory, antiarthritic, cyclooxygenase 2 inhibitor | 48 | — | — | — |
Ribavirin | Antiviral | 41 | 45 | — | 46 |
Tolbutamide | Antidiabetic | 45 | — | — | 22 |
Tranylcypromine sulfate | Antidepressant, monoamine oxidase inhibitor | 43 | — | — | — |
Diethylcarbamazine citrate | Anthelmintic | — | — | 43 | — |
Moxifloxacin hydrochloride | Antibacterial | 24 | 41 | — | 41 |
Tacrine hydrochloride | Anticholinesterase, cognitive adjuvant, K channel blocker | 40 | — | — | — |
Celecoxib | Antiarthritic, cyclooxygenase 2 inhibitor | 39 | — | 28 | — |
Propantheline bromide | Anticholinergic | — | 38 | — | — |
Orphenadrine citrate | Muscle relaxant (skeletal), antihistaminic | 38 | 28 | — | 45 |
Sulfanitran | Antibacterial | 37 | — | — | — |
Canrenone | Aldosterone antagonist, antifibrogenic | 37 | — | 33 | — |
Percentage of activation over baseline. The screening concentration for each compound was 10 μM. Values are expressed as the percentage of activity remaining over the baseline and are the average of two replicates. Positive hits were required to have duplicate data points ≥20% increase over baseline. Activity is calculated based on the metabolism of CYP-specific probe substrates to their respective metabolites. The compounds included in the table are representative of the diversity of the therapeutic areas and drug classes that exhibited heterotropic activation of CYP activity. Inhibition of enzymatic activity or no observed effect is designated with a dashed line.