Safety, Pharmacokinetics, and Pharmacodynamics of BIRT 2584 XX in Healthy Male Volunteers

Safety, Pharmacokinetics, and Pharmacodynamics of Single Rising Oral Doses of BIRT 2584 XX (5, 30, 100, 200, 350, 500, and 700 mg) as a Solution in PEG 400 Administered to Healthy Male Volunteers. Placebo Controlled and Blinded at Each Dose Level.

To assess safety, tolerability, pharmacokinetics, and pharmacodynamics of BIRT 2584 XX in single rising oral doses of 5 mg to 700 mg in a polyethylene glycol 400 (PEG 400) solution in healthy subjects

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Placebo; Drug: BIRT 2584 XX

• Study Type: Interventional
• Enrollment (Actual): 55
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 50 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Healthy male subjects as determined by results of screening
• Signed written informed consent in accordance with Good Clinical Practice (GCP) and local legislation
• Age >=18 and <=50 years
• BMI >=18.5 and <=29.9 kg/m2

Exclusion Criteria:

• Any finding of the medical examination (including blood pressure, pulse rate, and electrocardiogram) deviating from normal and of clinical relevance
• Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, haematological, 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) which is deemed relevant to the trial as judged by the investigator
• Intake of drugs with a long half-life (> 24 hours) (< 1 month prior to administration or during the trial)
• Use of any drugs, which might influence the results of the trial, (< 10 days prior to study drug administration or expected during the trial)
• Participation in another trial with an investigational drug (< 2 months prior to administration or expected during trial)
• Smoker (> 10 cigarettes or >3 cigars or >3 pipes/day)
• Alcohol abuse (> 60 g/day)
• Drug abuse
• Blood donation or loss > 400 mL, < 1 month prior to administration or expected during the trial
• Clinically relevant laboratory abnormalities
• Any ECG value outside of the reference range and of clinical relevance including, but not limited to QRS interval > 110 ms or QT interval, Bazett correction (QTcB) > 450 ms or QT interval >500 ms
• Inability to comply with dietary regimen of study centre
• Inability to comply with investigator's instructions

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Parallel Assignment
• Masking: Double

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Placebo Comparator: Placebo	Drug: Placebo
Experimental: BIRT 2584; single rising doses	Drug: BIRT 2584 XX

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Number of participants with adverse events	Up to 16 days after drug administration
Number of participants with clinically significant changes in vital signs	Up to 16 days after drug administration
Number of participants with abnormal changes in clinical laboratory parameters	Up to 16 days after drug administration
Number of participants with abnormal findings in 12-lead ECG (electrocardiogram)	Up to 16 days after drug administration
Number of participants with abnormal findings in physical examination	Screening and up to 16 days after drug administration

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cmax (maximum concentration in plasma)		Up to 360 hours after drug administration
tmax (time from dosing to maximum concentration)		Up to 360 hours after drug administration
AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time) interval from 0 extrapolated to infinity)		Up to 360 hours after drug administration
AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time) interval from 0 to the last quantifiable analyte plasma concentration)		Up to 360 hours after drug administration
λz (terminal rate constant in plasma)		Up to 360 hours after drug administration
t1/2 (terminal half-life of the analyte in plasma)		Up to 360 hours after drug administration
MRT(mean residence time of the analyte in the body)		Up to 360 hours after drug administration
CL/F (apparent oral clearance in plasma after oral administration)		Up to 360 hours after drug administration
Vz/F (apparent volume of distribution during the terminal phase λz) dose)		Up to 360 hours after drug administration
Ae0-48 (amount of analyte that is eliminated in urine from 0-48 hours)		Up to 48 hours after drug administration
fe0-48 (fraction of analyte eliminated in urine from 0-48 hours)		Up to 48 hours after drug administration
CLR,0-48 (renal clearance of the analyte from 0-48 hours)		Up to 48 hours after drug administration
Receptor occupancy as determined by binding of anti-LFA-1 antibody fragment (Fab)		Up to 360 hours after drug administration
Inhibition of IL-2 production	in response to superantigen challenge ex vivo	Up to 360 hours after drug administration

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim

Publications and helpful links

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start: March 1, 2004
• Primary Completion (Actual): June 1, 2004

Study Registration Dates

• First Submitted: October 7, 2014
• First Submitted That Met QC Criteria: October 7, 2014
• First Posted (Estimate): October 9, 2014

Study Record Updates

• Last Update Posted (Estimate): October 9, 2014
• Last Update Submitted That Met QC Criteria: October 7, 2014
• Last Verified: October 1, 2014

More Information

Terms related to this study

• Other Study ID Numbers: 1206.1