Drug intelligence / Profile preview

midazolam + omeprazole + tolbutamide

Development stage
Unknown
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Oral
01

Overview

This drug combination is a clinical research tool, specifically a 'probe cocktail' used in Phase 1 drug-drug interaction (DDI) studies. It consists of three distinct pharmaceutical agents: midazolam (a benzodiazepine), tolbutamide (a sulfonylurea), and omeprazole (a proton pump inhibitor). In the context of clinical development by Johnson & Johnson Pharmaceutical Research & Development, this combination was utilized to evaluate the inhibitory or inducing effects of investigational compounds, such as the antidepressant candidate JNJ-26489112, on specific Cytochrome P450 (CYP) enzymes. Specifically, midazolam serves as a probe for CYP3A4 activity, omeprazole for CYP2C19, and tolbutamide for CYP2C9. The combination itself is not a therapeutic treatment for major depressive disorder but is used to characterize the metabolic profile and potential safety risks of drugs being developed for that indication.

Other names
3-probe substrate drug combinationCYP probe cocktailDrug combination
02

Targets

CYP2C19 (Cytochrome P450 2C19)GABRR (GABA-A receptor subunit rho)ATP4A (Potassium–transporting ATPase alpha chain 1)KATP channel (ATP-sensitive potassium channel)CYP3A4 (Cytochrome P450 3A4)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)

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