Healthy
Conditions
Brief summary
Study to determine the safety, tolerability and pharmacokinetics of BILR 355 BS plus low dose ritonavir in healthy male volunteers.
Interventions
DRUGBILR 355 BS, solution
DRUGBILR 355 BS, tablet
DRUGRitonavir
DRUGPlacebo
Sponsors
Boehringer Ingelheim
Study design
Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
TREATMENT
Masking
DOUBLE
Eligibility
Sex/Gender
MALE
Age
18 Years to 59 Years
Healthy volunteers
Yes
Inclusion criteria
1. Males who meet the following criteria: Based upon a complete medical history, including the physical examination, vital signs (BP, PR), 12-lead ECG, clinical laboratory tests * No finding deviating from normal (except as noted below) and of clinical relevance * No evidence of a clinically relevant concomitant disease 2. Age ≥18 years and \<60 3. BMI ≥18.5 and BMI ≤29.9 kg/m2 (Body Mass Index) 4. Signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice and the local legislation
Exclusion criteria
1. Current and medically relevant gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders 2. Surgery of gastrointestinal tract (except appendectomy) 3. Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders 4. History of relevant orthostatic hypotension, fainting spells or blackouts 5. Chronic or relevant acute infections 6. History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator 7. Intake of drugs with a long half-life (\>24 hours) within one month prior to administration of study drug or during the trial 8. Use of drugs within 10 days prior to administration or during the trial, which might reasonably influence the results of the trial based on the knowledge at the time of protocol preparation 9. Participation in another trial with an investigational drug within one month prior to administration or during the trial 10. Smoker 11. Inability to refrain from smoking on trial days 12. Alcohol abuse (more than 60 g/day) 13. Drug abuse 14. Recent blood donation (more than 100 mL within 4 weeks prior to administration or during the trial) 15. Excessive physical activities (within 1 week prior to administration or during the trial) 16. Any laboratory value outside the normal reference range that is of clinical relevance 17. Inability to comply with dietary regimen of study centre 18. Infected with hepatitis B or hepatitis C viruses (defined as either being hepatitis B surface antigen, hepatitis B core antibody, or hepatitis C antibody positive) 19. HIV-1 infected as defined by a positive HIV ELISA test
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| AUCτ (area under the concentration time curve of BILR 355 in plasma over one dosing interval at steady state) | up to day 11 |
| Cmax (maximum concentration of BILR 355 in plasma) | up to day 11 |
| Time for BILR 355 BS to achieve steady state | up to day 11 |
| Cmin,ss (trough concentration of BILR 355 BS in plasma at steady state) | up to day 11 |
| Incidence of dose limiting toxicity | up to day 21 |
Secondary
| Measure | Time frame |
|---|---|
| tmax (time from dosing to the maximum concentration of BILR 355 in plasma) | up to day 11 |
| Number of subjects with adverse events | up to 42 days |
| AUCτ (area under the concentration time curve of metabolite 402 in plasma over one dosing interval at steady state) | up to day 11 |
| Cmax (maximum concentration of metabolite 402 in plasma) | up to day 11 |
| Ae (amount of BILR 355 excreted in the urine over the time interval from 0 to the time of the last urine collection interval) | up to day 11 |
| Metabolite BILR 402 Ae (amount of BILR 402 excreted in the urine over the time interval from 0 to the time of the last urine collection interval) | up to day 11 |
Outcome results
None listed