Study to Evaluate the Effect of Multiple Doses of BIRT 2584 XX Tablets on the Pharmacokinetic Parameters of Midazolam in Healthy Male Volunteers
Information source: Boehringer Ingelheim
ClinicalTrials.gov processed this data on August 23, 2015 Link to the current ClinicalTrials.gov record.
Condition(s) targeted: Healthy
Intervention: BIRT 2584 XX (Drug); Midazolam (Drug)
Phase: Phase 1
Status: Completed
Sponsored by: Boehringer Ingelheim
Summary
The objective of the study was to investigate the effect of BIRT 2584 XX and its metabolite
BI 610100 when BIRT 2584 XX is administered as a tablet to near steady state in estimated
high therapeutic dose on the pharmacokinetics (PK) of midazolam, a probe substrate for
CYP3A4. The PK of midazolam was measured before dosing of BIRT 2584 XX, after a single dose
of BIRT 2584 XX and after repeated doses of BIRT 2584 XX for 3 and 12 days
Clinical Details
Official title: A Study to Evaluate the Effect of Multiple Doses of 500 mg of BIRT 2584 XX Tablets on the Pharmacokinetic Parameters of Midazolam in Healthy Male Volunteers
Study design: Intervention Model: Single Group Assignment, Masking: Open Label, Primary Purpose: Treatment
Primary outcome: AUC0-∞ of midazolam (area under the concentration-time curve of midazolam in plasma over the time interval from 0 extrapolated to infinity)Cmax of midazolam (maximum concentration of midazolam in plasma) AUC0-∞ of 1'-hydroxymidazolam (area under the concentration-time curve of 1'-hydroxymidazolam in plasma over the time interval from 0 extrapolated to infinity) Cmax of 1'-hydroxymidazolam (maximum concentration of 1'-hydroxymidazolam in plasma) AUC0-∞ ratio of 1'-hydroxymidazolam to midazolam
Secondary outcome: AUC0-tz (area under the concentration-time curve of the analytes in plasma over the time interval from 0 to the time of the last quantifiable data point)tmax (time from dosing to the maximum concentration of the analytes in plasma) λz (terminal rate constant of the analytes in plasma) t1/2 (terminal half-life of the analytes in plasma) MRTpo (mean residence time of the analytes in the body after po administration) CL/F (apparent clearance of the analytes in the plasma after extravascular administration) Vz/F (apparent volume of distribution during the terminal phase following an extravascular dose) Pre-dose levels of BIRT 2584 XX and BI 610100 Number of subjects with abnormal findings in physical examination Number of subjects with abnormal changes in laboratory parameters Number of subjects with clinically significant changes in 12-lead ECG Number of subjects with clinically significant changes in vital signs Number of subjects with adverse events Assessment of tolerability by investigator on a 4-point scale
Eligibility
Minimum age: 18 Years.
Maximum age: 55 Years.
Gender(s): Male.
Criteria:
Inclusion Criteria:
- Healthy male subjects as determined by results of the screening
- Signed written informed consent in accordance with Good Clinical Practice (GCP) and
local legislation
- Age ≥ 18 and ≤ 55 years
- BMI ≥ 18. 5 and ≤ 29. 9 kg/m2
Exclusion Criteria:
- Any finding during the medical examination (including blood pressure, pulse rate, and
electrocardiogram) deviating from normal and of clinical relevance
- Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic,
immunologic, hematological, oncological, or hormonal disorders
- Surgery of gastrointestinal tract (except appendectomy)
- Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or
neurological disorders
- Relevant history of orthostatic hypotension, fainting spells, or blackouts
- Chronic or relevant acute infections
- History of allergy/hypersensitivity (including drug allergy) considered relevant to
the trial as judged by the investigator
- Intake of drugs with a long half-life (greater than 24 hours) (less than 1 month
prior to administration or during the trial)
- Use of any drugs, which might influence the results of the trial (less than 10 days
prior to study drug administration or expected during the trial)
- Participation in another trial with an investigational drug (less than 2 months prior
to administration or expected during trial)
- Smoker (more than 10 cigarettes/day or more than 3 cigars/day or more than 3
pipes/day)
- Alcohol abuse (more than 60 g of ethanol per day)
- Drug abuse
- Blood donation or loss greater than 400 mL (less than 1 month prior to administration
or expected during the trial)
- Clinically relevant laboratory abnormalities
Locations and Contacts
Additional Information
Starting date: June 2005
Last updated: October 2, 2014
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