CYP2C8 substrate, inhibitor, and inducer probes recommended for drug-drug interaction studies
| Probe | EMAa | FDAb | Helsinki DDI Group | |||
|---|---|---|---|---|---|---|
| In Vitro | In Vivo | In Vitro | In Vivo | In Vitro | In Vivo | |
| Substrate | Paclitaxel | Amodiaquine | Paclitaxelc | Repaglinide | Amodiaquine | Repaglinide |
| Amodiaquine | Repaglinide | Amodiaquine | Rosiglitazone | Paclitaxel | Montelukast | |
| Rosiglitazone | Montelukast | Pioglitazone | ||||
| Cerivastatin (acid) | Rosiglitazone | |||||
| (Pioglitazone) | (Dasabuvir) | |||||
| Inhibitor | Montelukast | Gemfibrozil | Montelukastc | Gemfibrozil | Montelukast | Gemfibrozil |
| Quercetinc | Gemfibrozil 1-O-β glucuronide | Clopidogrel | ||||
| Trimethoprim | Clopidogrel acyl 1-β-d-glucuronide | (Trimethoprim) | ||||
| Gemfibrozil | (Trimethoprim) | |||||
| Rosiglitazone | ||||||
| Pioglitazone | ||||||
| Inducer | None recommended | None recommended | Rifampin (rifampicin) | Rifampin (rifampicin) | Rifampin (rifampicin) | Rifampin (rifampicin) |
DDI, drug-drug interaction; EMA, European Medicines Agency; FDA, Food and Drug Administration.
↵a EMA, 2012b.
↵b http://www.fda.gov/Drugs/DevelopmentApprovalProcess/DevelopmentResources/DrugInteractionsLabeling/ucm093664.htm (Accessed September 15, 2015).
↵c Preferred.