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caffeine + dextromethorphan + omeprazole + midazolam + warfarin
- Development stage
- Preclinical
- Lead developer
- Novo Nordisk
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A Cytochrome P450 (CYP) phenotyping cocktail developed by Novo Nordisk for drug-drug interaction (DDI) assessment. This combination of five small molecule probe drugs—caffeine, dextromethorphan, omeprazole, midazolam, and warfarin—is administered orally to evaluate the activity of key drug-metabolizing enzymes: CYP1A2, CYP2D6, CYP2C19, CYP3A4, and CYP2C9, respectively. It serves as a diagnostic tool in clinical pharmacology to determine if an investigational new drug inhibits or induces these enzymes, thereby predicting potential interactions with other medications. By measuring the plasma concentrations of these probe drugs and their metabolites, researchers can establish a metabolic profile that informs the safety and dosing of new chemical entities.
- Other names
- Novo Nordisk CYP cocktailCYP phenotyping cocktailNovo Nordisk 5-drug cocktail
02
Targets
ADORA1 (Adenosine receptor A1 subtype)ADORA2A (Adenosine A₂A Receptor)BZD site (GABA-A receptor benzodiazepine site)ATP4A (Potassium–transporting ATPase alpha chain 1)NMDAR (Glutamate receptor ionotropic, NMDA)SIGMAR1 (Sigma non-opioid intracellular receptor 1)VKORC1 (Vitamin K epoxide reductase complex subunit 1)
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