A Study to Evaluate the Effect of Multiple Doses of 500 mg of BIRT 2584 XX Tablets on the Pharmacokinetic Parameters of Warfarin, Omeprazole, Caffeine, and Dextromethorphan Dosed Orally and Midazolam Dosed IV, in Healthy Male Volunteers

NCT02256813 Phase 1 COMPLETED

The study aimed to investigate the effect of BIRT 2584 XX and its metabolite BI 610100 on the Pharmacokinetics (PK) of five probe substrates for cytochrome P450 isozymes. The substrates used to monitor enzyme activity were oral warfarin (for CYP2C9), oral omeprazole (for CYP2C19), oral dextromethorphan (for CYP2D6), oral caffeine (for CYP1A2) and intravenous midazolam (for hepatic CYP3A)

Details

Lead sponsor	Boehringer Ingelheim
Phase	Phase 1
Status	COMPLETED
Enrolment	20
Start date	2005-09

Conditions

• Healthy

Interventions

• BIRT 2584 XX
• Warfarin sodium
• Omeprazole
• Dextromethorphan hydrobromide
• Caffeine
• Midazolam hydrochloride
• Vitamin K1

Primary outcomes

• AUC0-inf (Area under the concentration-time curve of midazolam IV and S-warfarin in plasma over the time interval from 0 extrapolated to infinity) — up to day 19
• AUC (Area under the concentration-time curve of the ratio of omeprazole to 5-hydroxyomeprazole in plasma) — up to day 19
• 0-12 hr urinary molar ratio of caffeine metabolites (1-Methylxanthine + 1-Methylurate +5-Acetylamino-6-formylamino-3-methyluracil)/ 1,7-Dimethylurate — up to 12 hours after administration
• 0-12 hr urinary dextromethorphan/dextrorphan ratio — up to 12 hours after administration