Clinical trial NCT02253927: Dose Escalation Study of Pharmacokinetics, Safety and Tolerability After Single Dose Administration of BILR 355 (SDS) Plus Low-dose Ritonavir in Healthy Volunteers
Official title: Phase I Sequential Dose Escalation Study of Pharmacokinetics, Safety and Tolerability After Single Dose (225 Mg-450 mg) Oral Administration of BILR 355 (SDS) Plus Low-dose Ritonavir in Healthy Volunteers
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Lead sponsor: Boehringer Ingelheim
Sponsor class: INDUSTRY
First posted: 2014-10-01
Enrollment: 48
Sex: ALL
Minimum age (years): 18
Maximum age (years): 60
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: NA
Intervention model: SINGLE_GROUP
Primary purpose: TREATMENT

Brief summary: The primary objective was to explore the relative bioavailability of increasing doses of BILR 355 BS, as a sodium dodecyl sulfate-containing solid formulation (SDS), in combination with ritonavir 100 mg and to explore the dose-concentration proportionality of increasing doses.

A secondary objective was to explore the effect of food on the pharmacokinetics of BILR 355 (SDS)


Eligibility criteria: Inclusion Criteria:

1. Males or females who met the inclusion/exclusion criteria, females who are not pregnant nor nursing, and who agreed to use a double-barrier method of birth control (condoms or diaphragm plus spermicide) throughout the trial (alone or in addition to other methods of birth control such as oral contraceptives)
2. Healthy HIV negative adult volunteers
3. Age ≥18 and ≤60 years
4. BMI ≥18.5 and BMI ≤29.9 kg/m2
5. Ability to give signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice (GCP) and the local regulations

Exclusion Criteria:

1. 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 at least one month prior to study drug administration and 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
9. Participation in another trial with an investigational drug within two months prior to administration or during the trial
10. Current smoker
11. Alcohol abuse (more than 60 g/day)
12. Drug abuse (positive urine test for illicit prescription or non-prescription drugs or drugs of abuse)
13. Blood donation (more than 100 mL within four weeks prior to study drug administration or during the trial)
14. Excessive physical activities (within one week prior to study drug administration or during the trial)
15. Any laboratory value outside the reference range that is of clinical relevance at screening, according to the judgment of the investigator
16. Inability to comply with dietary regimen required by the protocol
17. Infected with hepatitis B or hepatitis C viruses (defined as either being hepatitis B surface antigen, or hepatitis C antibody positive)
18. Pregnant or lactating females

Primary outcomes:
measure: AUC0-inf (Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)
timeFrame: up to 120 hours after drug administration
measure: Cmax (Maximum measured concentration of the analyte in plasma)
timeFrame: up to 120 hours after drug administration
measure: AUC0-tz (Area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the last quantifiable data point)
timeFrame: up to 120 hours after drug administration
measure: CL/F (Apparent clearance of the analyte in plasma following extravascular administration)
timeFrame: up to 120 hours after drug administration
measure: Tmax (Time from dosing to the maximum concentration of the analyte in plasma)
timeFrame: up to 120 hours after drug administration
measure: t½ (Terminal half-life of the analyte in plasma)
timeFrame: up to 120 hours after drug administration
Secondary outcomes:
measure: Number of patients with adverse events
timeFrame: up to 10 days after last dose administration
Other outcomes:
Locations:
Study officials:
References: