Safety/Tolerability, Pharmacokinetics, and Pharmacodynamics of BIBB 1464 MS in Healthy Male Subjects, Combined With Preliminary Evaluation of Relative Bioavailability and Effect of Food

Safety/Tolerability, Pharmacokinetics, and Pharmacodynamics of Single Oral Doses of 0.25 mg, 0.75 mg, 2 mg, 6 mg, and 10 mg BIBB 1464 MS (Tablet) in Healthy Male Subjects, Combined With Preliminary Evaluation of Relative Bioavailability and Effect of Food of the Dose of 0.75 mg or 2 mg or 6 mg (Two-stage Trial Design With Randomised Double Blind Placebo Controlled Rising Dose Phase and Subsequent Randomised, Open Parallel Group Phase)

Safety, pharmacodynamics and pharmacokinetics of 0.25, 0.75, 2.0, 6.0, and 10 mg BIBB 1464 p.o once daily in a rising dose group-comparison (placebo controlled, double blind, randomized per dose level).

Relative Bioavailability of 0.75 mg or 2 mg or 6 mg ( tablet vs. solution, intraindividual comparison), preliminary assessment of food effects (interindividual comparison)

Two-stage Trial Design With Randomised Double Blind Placebo Controlled Rising Dose Phase and Subsequent Randomised, Open Parallel Group Phase).

MS (Tablet) in Healthy Male Subjects, Combined With Preliminary Evaluation of Relative Bioavailability and Effect of Food of the Dose of 0.75 mg or 2 mg or 6 mg (Two-stage Trial Design With Randomised Double Blind Placebo Controlled Rising Dose Phase and Subsequent Randomised, Open Parallel Group Phase).

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: BIBB 1464 MS tablet; Other: Standard dinner; Drug: BIBB 1464 MS solution; Drug: BIBB 1464 MS placebo

• Study Type: Interventional
• Enrollment (Actual): 73
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 19 years to 54 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Healthy subjects as determined by results of screening
• Signed written informed consent in accordance with good clinical practice (GCP) and local legislation
• Age > 18 and < 55 years
• Broca > - 20% and < + 20%

Exclusion Criteria:

• Any findings of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance.
• Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal (including thyroid) disorder
• Surgery of the gastro-intestinal tract (except appendectomy)
• Disease of the central nervous system (such as epilepsy) or psychiatric 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) (<= 1 month prior to administration or during the trial)
• Use of any drugs which might influence the result of the trial (<= 10 days prior to administration or during the trial)
• Participation in another trial with an investigational drug (<= 2 month prior to administration or during the trial)
• Smoker (> 10 cigarettes or > 3 cigars or >3 pipes/day)
• Inability to refrain from smoking during the period of the study
• Known alcohol (>60 g/day) or drug abuse
• Blood donation (<=1 month prior to administration)
• Excessive physical activities (<5 days prior to administration)
• Any laboratory value outside the normal range of clinical relevance
• History of hemorrhagic diatheses
• History of gastro-intestinal ulcer, perforation or bleeding
• History of bronchial asthma

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
Experimental: BIBB 1464 MS single rising dose fed	Drug: BIBB 1464 MS tablet; Other: Standard dinner
Experimental: BIBB 1464 MS tablet fasted	Drug: BIBB 1464 MS tablet
Active Comparator: BIBB 1464 MS solution fasted	Drug: BIBB 1464 MS solution
Placebo Comparator: BIBB 1464 MS placebo	Drug: BIBB 1464 MS placebo

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Number of patients with adverse events	Up to 72 hours after last drug administration
Maximum drug plasma concentration (Cmax)	Up to 38 hours after drug administration
Time to reach the maximum concentration of the analyte in plasma (tmax)	Up to 38 hours after drug administration
Total area under the plasma drug concentration-time curve (AUC)	Up to 38 hours after drug administration
Apparent terminal half-life of the analyte in plasma (t1/2)	Up to 38 hours after drug administration
Total plasma clearance divided by the systemic availability factor (CL/f)	Up to 38 hours after drug administration
Dose normalized AUC0-38h ( NAUC0-38h)	Up to 38 h after drug administration
Mean residence time, total (MRTtot)	Up to 38 hours after drug administration
Number of patients with clinical significant findings in vital signs	Up to 38 hours after drug administration
Number of patients with clinical significant findings in electrocardiogram (ECG)	Up to 38 hours after drug administration
Number of patients with clinical significant findings in physical examination	Up to 38 hours after drug administration
Investigator assessed tolerability on a 4 point scale	Up to 38 hours after drug administration
Monoepoxysqualene (MES) plasma concentration	Up to 38 hours after drug administration
Amount of drug excreted in urine	Up to 38 h 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: July 1, 1999
• Primary Completion (Actual): September 1, 1999

Study Registration Dates

• First Submitted: August 28, 2014
• First Submitted That Met QC Criteria: August 28, 2014
• First Posted (Estimate): September 1, 2014

Study Record Updates

• Last Update Posted (Estimate): September 1, 2014
• Last Update Submitted That Met QC Criteria: August 28, 2014
• Last Verified: August 1, 2014

More Information

Terms related to this study

• Other Study ID Numbers: 1178.1