Clinical trial NCT02257008: Effect of Different Boosting Agents on Pharmacokinetics of BILR 355 BS Dissolved in Polyethylene Glycol 400 (PEG 400) in Healthy Male Volunteers
Official title: An Open Study to Investigate the Effect of Different Boosting Agents on Pharmacokinetics of Single Doses of BILR 355 BS (Dose Steps: 5 and 12.5 mg) Dissolved in 5 mL PEG 400 After Oral Administration in Healthy Male Volunteers
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Lead sponsor: Boehringer Ingelheim
Sponsor class: INDUSTRY
First posted: 2014-10-06
Enrollment: 44
Sex: MALE
Minimum age (years): 21
Maximum age (years): 50
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: PARALLEL
Primary purpose: TREATMENT

Brief summary: Assessment of the effect of different boosting agents on pharmacokinetics of a single dose of BILR 355 BS dissolved in PEG 400


Eligibility criteria: Inclusion Criteria:

* All participants in the study were to be healthy males, range from 21 to 50 years of age and their body mass index (BMI) be within 18.5 to 29.9 kg/m2 (BMI calculation: weight in kilograms divided by the square of height in meters)
* In accordance with good clinical practice (GCP) and the local legislation all volunteers had to give their written informed consent prior to admission to the study

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
* Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
* History of 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 by the investigator
* Intake of drugs with a long half-life (\> 24 hours) within at least one month or less than ten half-lives of the respective drug before enrolment in the study or during the study
* Use of any drugs which might influence the results of the trial up to 7 days prior to enrolment in the study or during the study
* Participation in another trial with an investigational drug (\<= two months prior to administration or during the trial)
* Smoker (\> 10 cigarettes or \> 3 cigars of \> 3 pipes/day)
* Inability to refrain from smoking on trial days
* Alcohol abuse (\> 60 g/day)
* Drug abuse
* Blood donation (\>= 100 mL within four weeks prior to administration or during the trial)
* Any laboratory value outside the clinically accepted reference range
* Excessive physical activities within the last week before the trial or during the trial

Following exclusion criteria are of special interest for this study:

* Erythema, exanthema and comparable skin alterations
* For the boosting agents atazanavir and atazanavir plus ritonavir, subjects with a PQ interval length in the screening ECG of \> 200 ms or any higher degree of atrio-ventricular (AV) block were to be excluded

Primary outcomes:
measure: Maximum observed concentration of the analyte in the plasma (Cmax)
timeFrame: up to 120 hours after start of treatment
measure: Time from dosing to the maximum concentration of the analyte in plasma (tmax)
timeFrame: up to 120 hours after start of treatment
measure: Area under the concentration-time curve of the analyte in plasma at different time points (AUC)
timeFrame: up to 120 hours after start of treatment
measure: Apparent terminal half-life of the analyte in plasma (t1/2)
timeFrame: up to 120 hours after start of treatment
measure: Apparent clearance of the analyte in plasma after extravascular multiple dose administration (CL/F)
timeFrame: up to 120 hours after start of treatment
measure: Total mean residence time of the analyte in the body (MRTtot)
timeFrame: up to 120 hours after start of treatment
measure: Apparent volume of distribution of the analyte during the terminal phase λz following extravascular administration (Vz/F)
timeFrame: up to 120 hours after start of treatment
measure: Renal clearance of the analyte determined over the dosing interval τ (CLR)
timeFrame: up to 120 hours after start of treatment
measure: Amount of the analyte excreted into urine (Ae)
timeFrame: up to 72 hours after start of treatment
Secondary outcomes:
measure: Number of participants with clinically relevant changes in laboratory parameters
timeFrame: up to 10 days after start of treatment
measure: Number of participants with clinically relevant changes in vital signs (blood pressure, pulse-, respiratory rate, body temperature)
timeFrame: up to 10 days after start of treatment
measure: Number of participants with clinically relevant changes in 12-lead ECG
timeFrame: up to 10 days after start of treatment
measure: Number of participants with clinically relevant changes in faecal occult blood testing
timeFrame: up to 10 days after start of treatment
measure: Number of participants with adverse events
timeFrame: Up to 25 days
measure: Global tolerability assessment by investigator on a 5-point scale
timeFrame: Up to 10 days after start of treatment
measure: Number of participants with clinically relevant changes in neurological assessment
timeFrame: up to 10 days after start of treatment
Other outcomes:
Locations:
Study officials:
References: