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

Boehringer Ingelheim

Status and phase: Completed; Phase 1

Conditions: Healthy

Treatments: Drug: Atazanavir; Drug: Nelfinavir; Other: Grapefruit juice; Drug: Ritonavir; Drug: BILR 355 BS

Study type: Interventional

Funder types: Industry

Identifiers

NCT02257008

1188.6

Details and patient eligibility

About

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

Enrollment: 44 patients

Sex: Male

Ages: 21 to 50 years old

Volunteers: Accepts Healthy Volunteers

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

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Parallel Assignment

Masking: None (Open label)

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44 participants in 4 patient groups

Single rising dose of BILR 355 BS with grapefruit juice

Experimental group

Treatment:

Other: Grapefruit juice

Drug: BILR 355 BS

Single rising dose of BILR 355 BS with nelfinavir

Experimental group

Treatment:

Drug: Nelfinavir

Drug: BILR 355 BS

Single dose of BILR 355 BS with atazanavir

Experimental group

Treatment:

Drug: Atazanavir

Drug: BILR 355 BS

Single dose of BILR 355 BS with atazanavir, ritonavir

Experimental group

Treatment:

Drug: Atazanavir

Drug: Ritonavir

Drug: BILR 355 BS