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