Clinical trial NCT02266485: Pharmacodynamics, Preliminary Pharmacokinetics and Tolerability of BIBB 515 BS or Pravastatin in Hyperlipemic Healthy Male Subjects
Official title: Pharmacodynamics, Preliminary Pharmacokinetics and Tolerability After Multiple Oral Doses of 2.5 mg o.d. BIBB 515 BS (Capsule) or Pravastatin 20 mg Over 2 Weeks in Hyperlipemic Healthy Male Subjects (Parallel Group Comparison, Randomized, Placebo Controlled, Partly Double Blind [Pravastatin Open])
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Lead sponsor: Boehringer Ingelheim
Sponsor class: INDUSTRY
First posted: 2014-10-17
Enrollment: 60
Sex: MALE
Minimum age (years): 18
Maximum age (years): 65
Standard ages: ADULT
OLDER_ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: PARALLEL
Primary purpose: TREATMENT

Brief summary: Investigation of pharmacodynamics (inhibition of oxidosqualene cyclase, MES as marker), effect on routine lipid profile parameters, safety and preliminary pharmacokinetics


Eligibility criteria: Inclusion Criteria:

* Healthy male caucasian subjects as determined by results of screening
* Written informed consent in accordance with good clinical practice (GCP) and local legislation given
* Age ≥ 18 and ≤ 65 years
* Broca ≥ - 20 % and ≤ + 30 %
* Cholesterol level ≥ 5.4 mmol/l

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 disorders
* Surgery of gastrointestinal tract (except appendectomy)
* Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurologic disorders
* History of orthostatic hypotension, fainting spells or blackouts
* Chronic or relevant acute infections
* History of allergy/hypersensitivity (including drug allergy) which was 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 administration or during the trial)
* Participation in another trial with an investigational drug (≤ 2 months prior to administration or during the trial)
* Smoker (\> 10 cigarettes or 3 cigars or 3 pipes/day)
* Inability to refrain from smoking on study days
* Alcohol abuse (\> 60 g/day)
* Drug abuse
* Blood donation \> 100 ml (≤ 4 weeks prior to administration or during the trial)
* Excessive physical activities (≤ 10 days prior to administration or during the trial)
* Any laboratory value outside the reference range of clinical relevance
* Abnormal findings at eye lens examination

Primary outcomes:
measure: Percentage changes in total-cholesterol
timeFrame: Pre-dose, up to day 15
measure: Percentage changes in low density lipoprotein (LDL) - cholesterol
timeFrame: Pre-dose, up to day 15
measure: Percentage changes in high density lipoprotein (HDL) - cholesterol
timeFrame: Pre-dose, up to day 15
measure: Percentage changes in apo-lipoprotein B
timeFrame: Pre-dose, up to day 15
measure: Percentage changes in lipoprotein (a)
timeFrame: Pre-dose, up to day 15
measure: Percentage changes in triglycerides
timeFrame: Pre-dose, up to day 15
measure: Maximum concentration of the analyte in plasma at different time points (Cmax)
timeFrame: Up 336 hours after first drug administration
measure: Time to reach maximum concentration of the analyte in plasma at different time points (tmax)
timeFrame: Up 336 hours after first drug administration
measure: Apparent terminal elimination half-life of the analyte in plasma (t1/2)
timeFrame: Up 336 hours after first drug administration
measure: Area under the concentration-time curve of the analyte in plasma at different time points (AUC)
timeFrame: Up 336 hours after first drug administration
measure: Total mean residence time of the analyte in the body (MRTtot)
timeFrame: Up 336 hours after first drug administration
measure: Apparent clearance of the analyte in plasma after extravascular multiple dose administration (CL/f)
timeFrame: Up 336 hours after first drug administration
measure: Apparent volume of distribution of the analyte during the terminal phase (Vz/f)
timeFrame: Up 336 hours after first drug administration
measure: Terminal rate constant of the analyte in plasma (λz)
timeFrame: Up 336 hours after first drug administration
measure: Number of participants with clinically relevant changes from baseline in physical examination
timeFrame: Pre-dose and day 15
measure: Number of participants with clinically relevant changes from baseline in 12-lead ECG
timeFrame: Pre-dose and day 15
measure: Number of participants with clinically relevant changes from baseline in lens examination
timeFrame: Pre-dose and day 15
measure: Number of participants with clinically relevant changes in vital signs (blood pressure, pulse rate, body weight)
timeFrame: Pre-dose, up to 324 hours after first drug administration
measure: Number of participants with clinically relevant changes in laboratory parameters
timeFrame: Pre-dose, up to 324 hours after first drug administration
measure: Number of participants with adverse events
timeFrame: Up to 1 day after last drug administration
measure: Global clinical assessment by the investigator
timeFrame: On day 15 after first drug administration
measure: Monoepoxy-squalene (MES) plasma concentration at different time points
timeFrame: Pre-dose, up to day 15
Secondary outcomes:
Other outcomes:
Locations:
Study officials:
References: