Safety, Tolerance, and Pharmacokinetics of BILN 2061 ZW in Healthy Male Subjects, Combined With Preliminary Evaluation of Food Effect

Safety, Tolerance, and Pharmacokinetics of Single Oral Doses of 5 mg, 20 mg, 60 mg, 100 mg, 200 mg, 400 mg, 600 mg, 800 mg, 1000 mg, 1200 mg, 1500 mg, 2000 mg and 2400 mg BILN 2061 ZW (PEG 400: Ethanol Solution) in Healthy Male Subjects, Combined With Preliminary Evaluation of Food Effect of the Dose of 200 mg (Two-Stage Trial Design With Randomised Double Blind Placebo Controlled Rising Dose Part and Subsequent Open Intraindividual Comparison Part)

To assess the safety, tolerance and pharmacokinetics of 5 mg to 2400 mg BILN 2061 ZW

1. In rising single doses
2. With and without a 64 g fat breakfast at one selected dose

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Placebo; Drug: BILN 2061 ZW single rising doses; Drug: BILN 2061 ZW fixed dose; Other: Standardized breakfast

• Study Type: Interventional
• Enrollment (Actual): 103
• 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
• Broca ≥ - 20 % and ≤ + 20 %

Exclusion Criteria:

• Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
• History or current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders, including a history of viral hepatitis, or serological evidence of active Hepatitis B or Hepatitis C infection
• History of orthostatic hypotension, fainting spells and blackouts
• Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
• 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) within 1 month prior to administration
• Use of any drugs which might influence the results of the trial within 10 days prior to administration or during the trial
• Participation in another trial with an investigational drug within 1 month prior to administration or during the trial
• Smoker (> 10 cigarettes or 3 cigars or 3 pipes/day) or inability to refrain from smoking on trial days
• Alcohol abuse (> 60 g/day)
• Drug abuse
• Blood donation within 1 month prior to administration or during the trial
• Excessive physical activities within 5 days prior to administration or during the trial
• Any laboratory value outside the clinically accepted reference range and of clinical relevance
• History of any familial bleeding disorder

Study Plan

How is the study designed?

Design Details

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

Number of Arms

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Placebo Comparator: Placebo	Drug: Placebo
Experimental: BILN 2061 ZW single rising doses	Drug: BILN 2061 ZW single rising doses
Experimental: BILN 2061 ZW fixed dose fed	Drug: BILN 2061 ZW fixed dose; Other: Standardized breakfast
Active Comparator: BILN 2061 ZW fixed dose fasted	Drug: BILN 2061 ZW fixed dose

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Number of patients with clinically relevant changes in vital signs (systolic and diastolic blood pressure, pulse rate)	Pre-dose, up to 48 hours after drug administration
Changes from baseline in laboratory tests	Pre-dose and 48 hours after drug administration
Number of patients with clinically relevant changes in 12-lead ECG	Pre-dose, up to 48 hours after drug administration
Changes from baseline in physical examination	Pre-dose and 48 hours after drug administration
Number of patients with adverse events	Up to 48 hours after drug administration
Global assessment of tolerability by the investigator on a 4-point scale	Up to 48 hours after drug administration
Maximum concentration of the analyte in plasma after a single dose administration (Cmax)	up to 48 hours after drug administration
Area under the concentration-time curve of the analyte in plasma from time 0 to infinity (AUC0-infinity)	up to 48 hours after drug administration
Time to reach Cmax following a single dose administration (tmax)	up to 48 hours after drug administration
Elimination half-life of the analyte in plasma (t1/2)	up to 48 hours after drug administration
Total oral clearance of the analyte from plasma after oral administration, divided by F (bioavailability factor) (CL/F)	up to 48 hours after drug administration
Total mean residence time of the analyte in plasma (MRT)	up to 48 hours after drug administration
Apparent volume of distribution during the terminal elimination phase (Vz/F)	up to 48 hours after drug administration
Amount of intact drug excreted in urine (Au)	up to 48 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: June 1, 2001
• Primary Completion (Actual): September 1, 2001

Study Registration Dates

• First Submitted: October 17, 2014
• First Submitted That Met QC Criteria: October 17, 2014
• First Posted (Estimate): October 20, 2014

Study Record Updates

• Last Update Posted (Estimate): October 20, 2014
• Last Update Submitted That Met QC Criteria: October 17, 2014
• Last Verified: October 1, 2014

More Information

Terms related to this study

• Other Study ID Numbers: 605.1