Pharmacokinetics of Single Doses of BILR 355 BS Given With Ritonavir in Healthy Male Volunteers

An Open Study to Investigate the Effect of Two Times Oral 100 mg Ritonavir Capsules 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, and a Double Blind, Placebo Controlled Study for Doses From 25 mg to 100 mg BILR 355 BS

Assessment of the effect of two times oral 100 mg ritonavir capsules on pharmacokinetics of a single dose of BILR 355 BS dissolved in PEG 400

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Placebo; Drug: Ritonavir; Other: high-fat breakfast; Drug: BILR 355 BS, D1; Drug: BILR 355 BS, D2; Drug: BILR 355 BS, D3; Drug: BILR 355 BS, D4; Drug: BILR 355 BS, D5; Drug: BILR 355 BS, D6; Drug: BILR 355 BS, D7; Drug: BILR 355 BS, D8; Drug: BILR 355 BS, D10

• Study Type: Interventional
• Enrollment (Actual): 62
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 21 years to 50 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• All participants in the study should be healthy males
• Age range from 21 to 50 years
• Body mass index (BMI) be within 18.5 to 29.9 kg/m2
• In accordance with Good Clinical Practice and the local legislation all volunteers will have given 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

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Parallel Assignment
• Masking: Double

Number of Arms

10

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: D10	Drug: Ritonavir; Other: high-fat breakfast; Drug: BILR 355 BS, D10
Experimental: D5	Drug: Ritonavir; Drug: BILR 355 BS, D5
Experimental: D1	Drug: Ritonavir; Drug: BILR 355 BS, D1
Experimental: D2	Drug: Ritonavir; Drug: BILR 355 BS, D2
Experimental: D3	Drug: Ritonavir; Drug: BILR 355 BS, D3
Experimental: D4	Drug: Ritonavir; Drug: BILR 355 BS, D4
Experimental: D6	Drug: Ritonavir; Drug: BILR 355 BS, D6
Experimental: D7	Drug: Ritonavir; Drug: BILR 355 BS, D7
Experimental: D8	Drug: Ritonavir; Drug: BILR 355 BS, D8
Placebo Comparator: Placebo; for D3 - D10	Drug: Placebo; Drug: Ritonavir

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Maximum observed concentration of the analyte in plasma (Cmax)	up to 120 hours after drug administration
Time to reach Cmax (tmax)	up to 120 hours after drug administration
Area under the concentration-time curve (AUC)	up to 120 hours after drug administration
Terminal half-life of the analyte in plasma (t1/2)	up to 120 hours after drug administration
Total clearance of the analyte in plasma (CL/F)	up to 120 hours after drug administration
Total mean residence time (MRTtot)	up to 120 hours after drug administration
Apparent volume of distribution (Vz/F)	up to 120 hours after drug administration
Renal clearance (CLR)	up to 72 hours after drug administration
Urinary excretion (Ae)	up to 72 hours after drug administration

Secondary Outcome Measures

Outcome Measure	Time Frame
Number of subjects with adverse events	up to 26 days

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim

Publications and helpful links

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start: November 1, 2002
• Primary Completion (Actual): December 1, 2003

Study Registration Dates

• First Submitted: September 30, 2014
• First Submitted That Met QC Criteria: September 30, 2014
• First Posted (Estimate): October 1, 2014

Study Record Updates

• Last Update Posted (Estimate): October 1, 2014
• Last Update Submitted That Met QC Criteria: September 30, 2014
• Last Verified: September 1, 2014

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Molecular Mechanisms of Pharmacological Action; Anti-Infective Agents; Antiviral Agents; Enzyme Inhibitors; Anti-HIV Agents; Anti-Retroviral Agents; Protease Inhibitors; Cytochrome P-450 CYP3A Inhibitors; Cytochrome P-450 Enzyme Inhibitors; HIV Protease Inhibitors; Viral Protease Inhibitors; Ritonavir
• Other Study ID Numbers: 1188.4