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caffeine + dextromethorphan + flurbiprofen + midazolam + omeprazole
- Development stage
- Phase 1
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
The CYP450 Drug Cocktail is an orally administered diagnostic probe cocktail consisting of caffeine, dextromethorphan, flurbiprofen, midazolam, and omeprazole. It is utilized in clinical pharmacology studies to simultaneously evaluate the metabolic activity of five major human cytochrome P450 (CYP) enzymes: CYP1A2 (probed by caffeine), CYP2D6 (probed by dextromethorphan), CYP2C9 (probed by flurbiprofen), CYP3A4/5 (probed by midazolam), and CYP2C19 (probed by omeprazole). By administering sub-therapeutic doses of these probe substrates, researchers can assess the potential of investigational drugs (such as Eli Lilly's SARM1 inhibitor LY3873862) to inhibit or induce these key drug-metabolizing enzymes, thereby characterizing potential drug-drug interactions.
- Other names
- 5-drug phenotyping cocktailCYP450 Drug CocktailCYP-450 Drug CocktailCYP 450 Drug CocktailCYP450 cocktailCYP-450 cocktailCYP 450 cocktailcytochrome P450 drug cocktail
02
Targets
ATP4A (Potassium–transporting ATPase alpha chain 1)CYP1A2 (Cytochrome P450 1A2)CYP2C19 (Cytochrome P450 2C19)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP2D6 (Cytochrome P450 2D6)CYP3A4 (Cytochrome P450 3A4)CYP3A5 (Cytochrome P450 family 3 subfamily A member 5)
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