Drug intelligence / Profile preview

ethanol + caffeine + tolbutamide + omeprazole + dextromethorphan + digoxin + midazolam

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of six drugs—ethanol, caffeine, tolbutamide, omeprazole, dextromethorphan, digoxin, and midazolam—administered together as a "six-probe cocktail." The primary use of this combination is not for therapeutic purposes but as a pharmacokinetic tool in clinical research to simultaneously assess the activity of multiple drug-metabolizing enzymes (notably cytochrome P450 isoforms) and transporters in vivo. Each component serves as a probe substrate for specific metabolic pathways or transporters: - Caffeine (CYP1A2 substrate) - Tolbutamide (CYP2C9 substrate) - Omeprazole (CYP2C19 substrate) - Dextromethorphan (CYP2D6 substrate) - Midazolam (CYP3A4 substrate) - Digoxin (P-glycoprotein transporter probe) - Ethanol may be included to assess alcohol metabolism or interactions. The cocktail approach allows researchers to phenotype an individual's drug metabolism capacity and transporter function efficiently. This method supports personalized medicine by identifying genetic variations that affect drug disposition[1].

Other names
six-probe cocktail6-probe cocktail
02

Targets

CYP2C19 (Cytochrome P450 2C19)CYP1A2 (Cytochrome P450 1A2)ADH (Alcohol dehydrogenase family)ABCB1 (P-glycoprotein)CYP3A4 (Cytochrome P450 3A4)CYP2E1CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP3A7 (Cytochrome P450 3A7)CYP3A5 (Cytochrome P450 family 3 subfamily A member 5)

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