Clinical trial NCT01605461: Study Evaluating Absorption, Distribution, Metabolism and Excretion (ADME) of Single Dose [14C]-BI 207127 in Healthy Male Volunteers
Official title: Metabolite Profile, Excretion Balance and Pharmacokinetics of BI 207127 NA Combined With [14C]-BI 207127 NA in Healthy Adult Male Volunteers After an 800 mg Single Oral Solution Dose; a Phase I, Single-arm, Open-label Trial
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Lead sponsor: Boehringer Ingelheim
Sponsor class: INDUSTRY
First posted: 2012-05-25
Enrollment: 12
Sex: MALE
Minimum age (years): 18
Maximum age (years): 55
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: NA
Intervention model: SINGLE_GROUP
Primary purpose: BASIC_SCIENCE

Brief summary: Phase 1 study to assess the pharmacokinetics and routes of elimination of a single oral dose of \[14C\]-BI 207127 and to characterize the metabolic profile following single dose administration.


Eligibility criteria: Inclusion criteria:

* Body mass index =18.5 and BMI = 29.9 kg/m2
* Subject is willing to avoid sun exposure from the first administration of the trial drug until the end of the study
* Male subjects must agree to minimise the risk of female partners becoming pregnant from the dosing day until three months after the completion of the study. Acceptable methods of contraception for male volunteers include a vasectomy no less than three months prior to dosing or barrier contraception. For female partners of male volunteers, acceptable methods of contraception include intra-uterine device, tubal ligation, or hormonal contraceptive for at least three months, or diaphragm with spermicide.
* Signed and dated written informed consent prior to admission to the study in accordance with GCP and the local legislation.

Exclusion criteria:

* Participation in more than one other radiolabelled investigational study drug trial within 12 months prior to check-in. The previous radiolabelled study drug must have been received more than 6 months prior to check-in for this study and the total exposure from this study and the previous study will be within the recommended levels considered safe, per 21 CFR 361.1 (eg. less than 5,000 mrem whole body annual exposure)
* Exposure to significant radiation (eg. serial x-ray or computed tomography scans, barium meal, current employment in a job requiring radiation exposure monitoring) within 12 months prior to check-in
* Participation in another trial with an investigational drug within two months prior to administration of the trial drug or during the trial
* Use of drugs which might reasonably influence the results of the trial, including use of a broad spectrum antibiotic, within 10 days prior to administration of investigational medication in this trial or during the trial
* Intake of a drug with a half-life of \>24 hours within the month prior to administration of trial medication, or if administration of trial medication would occur in the time period in which fewer than 10 half-lives had elapsed
* Surgery of the gastrointestinal tract (except appendectomy or cholecystectomy)
* Current smoker or smoker in last six months; alcohol abuse (more than 40 g/day); history of illicit drug abuse within the past 2 years
* Blood donation (more than 100 mL within four weeks prior to first administration of the trial drug or during the trial)
* A marked baseline prolongation of QT/QTc interval (e.g., repeated demonstration of a QTc interval \>450 ms); a history of additional risk factors for torsades de pointes (TdP) (e.g., heart failure, hypokalemia, family history of Long QT Syndrome)
* History of photosensitivity or recurrent rash
* Irregular defecation pattern (less than one bowel movement a day)

Primary outcomes:
measure: AUC0-infinity of Plasma Deleobuvir
timeFrame: 15 minutes (min) before drug administration and 30min, 1 hour (h), 1h 30min, 2h, 2h 30min, 3h, 3h 30min, 4h, 5h, 6h, 8h, 10h, 12h, 15h, 24h, 36h, 48h, 72h and 96h after drug administration
measure: Cmax of Plasma Deleobuvir
timeFrame: 15 minutes (min) before drug administration and 30min, 1 hour (h), 1h 30min, 2h, 2h 30min, 3h, 3h 30min, 4h, 5h, 6h, 8h, 10h, 12h, 15h, 24h, 36h, 48h, 72h and 96h after drug administration
measure: t1/2 of [14C]-Radioactivity in Plasma
timeFrame: 15 minutes (min) before drug administration and 30min, 1 hour (h), 1h 30min, 2h, 2h 30min, 3h, 3h 30min, 4h, 5h, 6h, 8h, 10h, 12h, 15h, 24h, 36h, 48h, 72h and 96h after drug administration
measure: Excretion Balance of Total [14C]-Radioactivity
timeFrame: Before drug administration (24hours (h) to 15 minutes pre-dose) and 0h-24h, 24h-48h, 48h-72h, 72h-96h, 96h-120h, 120h-144h, 144h-168h, 168h-192h and 192h-216h after drug administration
measure: Excretion of Total [14C]-Radioactivity in Urine
timeFrame: Before drug administration (24hours (h) to 15 minutes pre-dose) and 0h-24h, 24h-48h, 48h-72h, 72h-96h, 96h-120h, 120h-144h, 144h-168h, 168h-192h and 192h-216h after drug administration
measure: Excretion of Total [14C]-Radioactivity in Faeces
timeFrame: Before drug administration (24hours (h) to 15 minutes pre-dose) and 0h-24h, 24h-48h, 48h-72h, 72h-96h, 96h-120h, 120h-144h, 144h-168h, 168h-192h and 192h-216h after drug administration
Secondary outcomes:
Other outcomes:
Locations:
city: Madison
country: United States
facility: 1241.22.001 Boehringer Ingelheim Investigational Site
state: Wisconsin
Study officials:
affiliation: Boehringer Ingelheim
name: Boehringer Ingelheim
role: STUDY_CHAIR
References: