Pharmacodynamics, Preliminary Pharmacokinetics and Tolerability of BIBB 1464 (Tablet) in Hyperlipemic Healthy Male Subjects

August 28, 2014 updated by: Boehringer Ingelheim

Pharmacodynamics, Preliminary Pharmacokinetics and Tolerability After Multiple Oral Doses of 0.25 mg, 0.5 mg and 1 mg o.d. BIBB 1464 (Tablet) or Pravastatin 20 mg Over 2 Weeks in Hyperlipemic Healthy Male Subjects (Parallel Group Comparison, Randomized, Placebo Controlled, Partly Double Blind [Pravastatin Open])

Lipid lowering effect, investigation of pharmacodynamics (inhibition of oxidosqualene cyclase, monoepoxysqualene (MES) as marker), safety / tolerability and preliminary pharmacokinetics

Study Overview

Study Type

Interventional

Enrollment (Actual)

100

Phase

  • Phase 1

Participation Criteria

Researchers look for people who fit a certain description, called eligibility criteria. Some examples of these criteria are a person's general health condition or prior treatments.

Eligibility Criteria

Ages Eligible for Study

18 years to 65 years (Adult, Older Adult)

Accepts Healthy Volunteers

Yes

Genders Eligible for Study

Male

Description

Inclusion Criteria:

  • Healthy male Caucasian subjects as determined by results of screening
  • Written informed consent in accordance with GCP and local legislation given
  • Age >= 18 and <= 65 years
  • Broca >= - 20% and <= + 30%
  • LDL-cholesterol level >= 3.3 mmol/L at pre-screening and at the two screening visits

Exclusion Criteria:

  • Any finding 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 or neurological disorders
  • History or 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 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
  • Alcohol abuse (>60/g/day)
  • Drug abuse
  • Blood donation (>400ml <=1 month prior to administration)
  • Excessive physical activities (<=5 days prior to administration)
  • Any laboratory value outside the normal range of clinical relevance
  • LDL - cholesterol screening measurements day -1 and day -7 the different between these two values exceed 12% of the higher dose
  • subjects who are vegetarian

Eye-lens

  • Cataract extraction in one or both eyes deemed likely within 2 years ("senile", non-idiopathic will not automatically exclude patients from participation)
  • Lens Opacities Classification System (LOCS) III grade >3.0 (for nuclear opalescence or cortical grad) >0.5 (for posterior sub capsular grad)
  • Log MAR Bailey-Lovie visual acuity >0.5
  • Corneal or conjunctival problems which would preclude lens photography
  • Shallow anterior chamber with risk of angle-closure glaucoma
  • Pupil will not dilate to at least 6 mm
  • Visually significant fundus pathology in clinician's judgment
  • Amblyopia, optic nerve disease, iritis, history of eye surgery, argon or YAG laser, major eye trauma, extended use (daily for >3 month) of ocular or systemic corticosteroid treatment , use of anticoagulants, or glaucoma therapy, or participation in another clinical trial investigation an anti-cataract or cataractogenic formulation within the last year

Study Plan

This section provides details of the study plan, including how the study is designed and what the study is measuring.

How is the study designed?

Design Details

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

Arms and Interventions

Participant Group / Arm
Intervention / Treatment
Placebo Comparator: Placebo
Active Comparator: Pravastatin
Experimental: BIBB 1464 MS low dose
Experimental: BIBB 1464 MS medium dose
Experimental: BIBB 1464 MS high dose

What is the study measuring?

Primary Outcome Measures

Outcome Measure
Time Frame
Percentage change of LDL plasma cholesterol
Time Frame: baseline, 2 weeks
baseline, 2 weeks
Percentage change of total plasma cholesterol
Time Frame: baseline, 2 weeks
baseline, 2 weeks

Secondary Outcome Measures

Outcome Measure
Time Frame
Percentage change in lipid profile
Time Frame: baseline, 1 week
baseline, 1 week
Number of patients with adverse events
Time Frame: Up to day 42
Up to day 42
Number of patients with clinical significant findings in eye lens opacification
Time Frame: Up to day 42
Up to day 42
Number of patients with clinical significant findings in laboratory parameters
Time Frame: Up to day 28
Up to day 28
Number of patients with clinical significant findings in electrocardiogram (ECG)
Time Frame: Up to day 28
Up to day 28
Number of patients with clinical significant findings in physical examination
Time Frame: Up to day 28
Up to day 28
Number of patients with clinical significant findings in vital signs
Time Frame: Up to day 15
Up to day 15
Investigator assessed tolerability on a 4 point scale
Time Frame: day 42
day 42
Amount of drug excreted in urine
Time Frame: Up to day 15
Up to day 15
Drug plasma concentration
Time Frame: Up to day 28
Up to day 28
Monoepoxysqualene (MES) plasma concentration
Time Frame: Up to day 28
Up to day 28

Collaborators and Investigators

This is where you will find people and organizations involved with this study.

Publications and helpful links

The person responsible for entering information about the study voluntarily provides these publications. These may be about anything related to the study.

Helpful Links

Study record dates

These dates track the progress of study record and summary results submissions to ClinicalTrials.gov. Study records and reported results are reviewed by the National Library of Medicine (NLM) to make sure they meet specific quality control standards before being posted on the public website.

Study Major Dates

Study Start

January 1, 2000

Primary Completion (Actual)

May 1, 2000

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

This information was retrieved directly from the website clinicaltrials.gov without any changes. If you have any requests to change, remove or update your study details, please contact register@clinicaltrials.gov. As soon as a change is implemented on clinicaltrials.gov, this will be updated automatically on our website as well.

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