Effect of Different Boosting Agents on Pharmacokinetics of BILR 355 BS Dissolved in Polyethylene Glycol 400 (PEG 400) in Healthy Male Volunteers

NCT02257008 | Completed Phase 1

• 1 other identifier: 1188.6
• Study Type: interventional
• Target: 44
• Locations: 0 countries
• Sites: N/A

Brief Summary

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

Conditions

Healthy

Outcome Measures

Primary Outcomes (9)

• Maximum observed concentration of the analyte in the plasma (Cmax)

  up to 120 hours after start of treatment

• Time from dosing to the maximum concentration of the analyte in plasma (tmax)

  up to 120 hours after start of treatment

• Area under the concentration-time curve of the analyte in plasma at different time points (AUC)

  up to 120 hours after start of treatment

• Apparent terminal half-life of the analyte in plasma (t1/2)

  up to 120 hours after start of treatment

• Apparent clearance of the analyte in plasma after extravascular multiple dose administration (CL/F)

  up to 120 hours after start of treatment

• Total mean residence time of the analyte in the body (MRTtot)

  up to 120 hours after start of treatment

• Apparent volume of distribution of the analyte during the terminal phase λz following extravascular administration (Vz/F)

  up to 120 hours after start of treatment

• Renal clearance of the analyte determined over the dosing interval τ (CLR)

  up to 120 hours after start of treatment

• Amount of the analyte excreted into urine (Ae)

  up to 72 hours after start of treatment

Secondary Outcomes (7)

• Number of participants with clinically relevant changes in laboratory parameters

  up to 10 days after start of treatment

• Number of participants with clinically relevant changes in vital signs (blood pressure, pulse-, respiratory rate, body temperature)

  up to 10 days after start of treatment

• Number of participants with clinically relevant changes in 12-lead ECG

  up to 10 days after start of treatment

• Number of participants with clinically relevant changes in faecal occult blood testing

  up to 10 days after start of treatment

• Number of participants with adverse events

  Up to 25 days

Study Arms (4)

Single rising dose of BILR 355 BS with grapefruit juice

EXPERIMENTAL

Drug: BILR 355 BS; Other: Grapefruit juice

Single rising dose of BILR 355 BS with nelfinavir

EXPERIMENTAL

Drug: BILR 355 BS; Drug: Nelfinavir

Single dose of BILR 355 BS with atazanavir

EXPERIMENTAL

Drug: BILR 355 BS; Drug: Atazanavir

Single dose of BILR 355 BS with atazanavir, ritonavir

EXPERIMENTAL

Drug: BILR 355 BS; Drug: Atazanavir; Drug: Ritonavir

Interventions

BILR 355 BS DRUG

Single dose of BILR 355 BS with atazanavir; Single dose of BILR 355 BS with atazanavir, ritonavir; Single rising dose of BILR 355 BS with grapefruit juice; Single rising dose of BILR 355 BS with nelfinavir

Grapefruit juice OTHER

Single rising dose of BILR 355 BS with grapefruit juice

Nelfinavir DRUG

Single rising dose of BILR 355 BS with nelfinavir

Atazanavir DRUG

Single dose of BILR 355 BS with atazanavir; Single dose of BILR 355 BS with atazanavir, ritonavir

Ritonavir DRUG

Single dose of BILR 355 BS with atazanavir, ritonavir

Eligibility Criteria

• Age: 21 Years - 50 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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

Sponsors & Collaborators

• Boehringer Ingelheim: lead

MeSH Terms

Interventions

Nelfinavir; Atazanavir Sulfate; Ritonavir

Intervention Hierarchy (Ancestors)

Isoquinolines; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds; Pyridines; Heterocyclic Compounds, 1-Ring; Oligopeptides; Peptides; Amino Acids, Peptides, and Proteins; Thiazoles; Sulfur Compounds; Organic Chemicals; Azoles

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: October 2, 2014
• First Posted: October 6, 2014
• Study Start: March 1, 2003
• Primary Completion: December 1, 2003
• Last Updated: October 6, 2014

Record last verified: 2014-10