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

Recruitment & Eligibility

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 & Design

Arm && Interventions

Primary Outcome Measures

Name	Time	Method
Percentage change of total plasma cholesterol	baseline, 2 weeks
Percentage change of LDL plasma cholesterol	baseline, 2 weeks

Secondary Outcome Measures

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

Recruitment & Eligibility