Drug intelligence / Profile preview

warfarin + caffeine + midazolam

Development stage
Unknown
Lead developer
Novo Nordisk
Modality
Small Molecules
Administration
Oral
01

Overview

The combination of warfarin, caffeine, and midazolam is a drug-drug interaction (DDI) probe cocktail used in clinical pharmacology to evaluate the metabolic activity of specific Cytochrome P450 (CYP) enzymes. In this cocktail, caffeine serves as a probe for CYP1A2, warfarin (specifically the S-enantiomer) is a probe for CYP2C9, and midazolam is a probe for CYP3A4/5. This combination is frequently employed in Phase 1 clinical trials, such as those conducted by Novo Nordisk for the triple agonist UBT251, to determine if an investigational therapeutic candidate induces or inhibits these key hepatic metabolic pathways. By measuring the pharmacokinetics of these index substrates, researchers can assess the potential for the new drug to cause clinically significant interactions with other medications metabolized by the same enzymes.

Other names
CYP enzyme probe substratesCYP cocktail
02

Targets

ADORA1 (Adenosine receptor A1 subtype)ADORA2A (Adenosine A₂A Receptor)CYP1A2 (Cytochrome P450 1A2)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP3A4 (Cytochrome P450 3A4)GABA-A α/γ interface (Gamma-aminobutyric acid type A receptor (GABA-A receptor) alpha/gamma subunit interface)VKORC1 (Vitamin K epoxide reductase complex subunit 1)

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