Drug intelligence / Profile preview

caffeine + pioglitazone + flurbiprofen + omeprazole + dextromethorphan + midazolam + rosuvastatin

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

Overview

This is a **combination formulation** of six small molecule pharmaceuticals with distinct pharmacological mechanisms: - **Caffeine**: A central nervous system stimulant and adenosine receptor antagonist, commonly found in beverages, with documented effects on alertness and metabolism. - **Pioglitazone**: A thiazolidinedione antidiabetic agent that acts as an agonist at peroxisome proliferator-activated receptor gamma, improving insulin sensitivity, mainly for type 2 diabetes. - **Flurbiprofen**: A non-steroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2), reducing prostaglandin synthesis and inflammation. - **Omeprazole**: A proton pump inhibitor that blocks gastric H+/K+ ATPase, reducing gastric acid secretion, commonly used for gastroesophageal reflux disease and peptic ulcers. - **Dextromethorphan**: An antitussive and non-competitive NMDA receptor antagonist used for cough suppression and with additional activity at several other central targets. - **Midazolam**: A benzodiazepine, positive allosteric modulator of the GABA-A receptor, used as a sedative and anxiolytic. - **Rosuvastatin**: An HMG-CoA reductase inhibitor (statin) that lowers cholesterol by inhibiting the rate-limiting step in cholesterol biosynthesis. This combination does **not match any single marketed product** and is likely used as a pharmacokinetic cocktail (probe drugs) to assess the activity of several CYP450 enzymes (CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4) and drug-drug interactions in clinical pharmacology research. There are documented pharmacokinetic and pharmacodynamic interactions among some component drugs, such as caffeine increasing pioglitazone bioavailability and omeprazole affecting metabolism of certain other drugs[1][4][3].

02

Targets

ADORA2A (Adenosine A₂A Receptor)GABRA2 (Gamma-aminobutyric acid receptor subunit alpha 2)ADORA1 (Adenosine receptor A1 subtype)ATP4A (Potassium–transporting ATPase alpha chain 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PPARG (Peroxisome proliferator-activated receptor gamma)PGHS-1 (Prostaglandin G/H Synthase 1)SIGMAR1 (Sigma non-opioid intracellular receptor 1)NMDAR (Glutamate receptor ionotropic, NMDA)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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