caffeine + montelukast + midazolam

This drug cocktail is a combination of three probe substrates—caffeine (200 mg), montelukast (10 mg), and midazolam (4 mg)—used by H. Lundbeck A/S in clinical pharmacology studies. It was specifically employed in a Phase 1 trial (NCT03162874) to evaluate the potential for drug-drug interactions (DDI) between these substrates and foliglurax (Lu AF99757), an investigational metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulator. In this context, caffeine serves as a probe for Cytochrome P450 1A2 (CYP1A2) activity, montelukast for CYP2C8, and midazolam for CYP3A4. The cocktail allows researchers to determine if the co-administered drug (foliglurax) inhibits or induces these specific metabolic pathways. While the cocktail itself is a diagnostic tool, the development program for foliglurax in Parkinson's disease was ultimately terminated following disappointing Phase 2 results.

Other names

Drug CocktailCYP450 probe cocktailCYP-450 probe cocktailCYP 450 probe cocktailcaffeine/montelukast/midazolam cocktail