Clinical cocktails for cytochrome P450 (CYP) phenotyping lack a marker for CYP2C8. We aimed to combine the CYP2C8 index drug repaglinide with the Geneva cocktail (caffeine/CYP1A2, bupropion/CYP2B6, flurbiprofen/CYP2C9, omeprazole/CYP2C19, dextromethorphan/CYP2D6, and midazolam/CYP3A4). We also included endogenous organic anion transporting polypeptide (OATP) 1B1 and 1B3 biomarkers glycochenodeoxycholate 3-O-glucuronide and glycochenodeoxycholate 3-sulfate, and investigated the CYP2C8 inhibition selectivity of clopidogrel and gemfibrozil with the full cocktail. In a five-phase randomized cross-over study, the following drugs were administered to 16 healthy volunteers: (i) repaglinide, (ii) the Geneva cocktail, (iii) repaglinide with the Geneva cocktail (full cocktail), (iv) clopidogrel followed by the full cocktail, and (v) gemfibrozil followed by the full cocktail. The Geneva cocktail increased repaglinide AUC