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caffeine + tolbutamide + dextromethorphan + midazolam + digoxin
- Development stage
- Unknown
- Lead developer
- Michael Hoelscher
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
This probe drug cocktail is a specific combination of five drugs—caffeine, tolbutamide, dextromethorphan, midazolam, and digoxin—used as a diagnostic tool in clinical pharmacology to evaluate the activity of key metabolic enzymes and transporters. In the Phase Ib/IIa clinical trial led by Michael Hoelscher for the treatment of pulmonary tuberculosis, this cocktail is employed to assess potential drug-drug interactions (DDI) between the investigational drug BTZ-043 and Cytochrome P450 enzymes (CYP1A2, CYP2C9, CYP2D6, CYP3A4) and the P-glycoprotein (P-gp) transporter. By measuring the plasma concentrations of these probe substrates and their metabolites, researchers can determine if BTZ-043 inhibits or induces these pathways, which is critical for establishing the safety and dosing profile of the new anti-tuberculosis agent.
- Other names
- probe drug cocktail-Michael Hoelscher-pulmonary tuberculosisProbe Drug Cocktail
02
Targets
CYP1A2 (Cytochrome P450 1A2)CYP3A4 (Cytochrome P450 3A4)ABCB1 (P-glycoprotein)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)
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