Drug intelligence / Profile preview

midazolam + omeprazole + dextromethorphan

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

Overview

This is a combination of three pharmaceutical agents—midazolam, omeprazole, and dextromethorphan—commonly used as part of a multi-drug "cocktail" to assess the activity of various cytochrome P450 (CYP) drug-metabolizing enzymes in clinical pharmacokinetic studies. Each component serves as a probe substrate for specific CYP enzymes: - Midazolam is primarily metabolized by CYP3A4 and is used to assess CYP3A activity. - Omeprazole is metabolized mainly by CYP2C19 and serves as a probe for this enzyme. - Dextromethorphan is metabolized by CYP2D6 and acts as its probe substrate. The combination allows simultaneous evaluation of multiple metabolic pathways in vivo, supporting research into drug interactions, genetic polymorphisms affecting metabolism, and personalized medicine approaches. This cocktail does not have therapeutic intent but rather serves as an investigative tool in clinical pharmacology[1][2][3].

Other names
six-probe cocktail
02

Targets

CYP3A4 (Cytochrome P450 3A4)GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)CYP2D6 (Cytochrome P450 2D6)CYP2C19 (Cytochrome P450 2C19)

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