A Phase I Trial to Investigate the Metabolism and Pharmacokinetics as Well as Safety and Tolerability of a Single Dose BI671800 HEA Administered as an Oral Solution of the Choline Salt in Healthy Male Volunteers

This study has been completed.
Sponsor:
Information provided by:
Boehringer Ingelheim
ClinicalTrials.gov Identifier:
NCT01205373
First received: September 17, 2010
Last updated: October 31, 2013
Last verified: October 2013
  Purpose

The main objectives of the present study are to investigate the basic pharmacokinetics of BI 671800, its major metabolite CD6384, and 14C-radioactivity, including mass balance, excretion pathways and metabolism following a single oral dose of 400 mg [14C]BI 671800 HEA to healthy male volunteers. Secondary objectives are to evaluate the safety and tolerability following a single oral dose of 400 mg [14C]BI 671800 HEA to healthy male volunteers.


Condition Intervention Phase
Healthy
Drug: BI 671800
Phase 1

Study Type: Interventional
Study Design: Allocation: Non-Randomized
Endpoint Classification: Pharmacokinetics Study
Intervention Model: Single Group Assignment
Masking: Open Label
Primary Purpose: Treatment
Official Title: A Phase I Trial to Investigate the Metabolism and Pharmacokinetics of an Open-label Single Dose of 400 mg [14C]BI 671800 HEA Administered as an Oral Solution of the Choline Salt in Healthy Male Volunteers.

Resource links provided by NLM:


Further study details as provided by Boehringer Ingelheim:

Primary Outcome Measures:
  • Individual time course profiles of 14C-radioactivity (in nmol eq/L or nmol eq/kg for faeces) in whole blood, plasma, urine, and faeces [ Time Frame: up to 336 h post treatment ] [ Designated as safety issue: No ]
  • Individual time course profiles of BI 671800 and its major metabolite CD6384 in plasma and urine [ Time Frame: up to 336 h post treatment ] [ Designated as safety issue: No ]
  • Rate and extent of excretion mass balance based on the total radioactivity in urine and faeces [ Time Frame: up to 336 h post treatment ] [ Designated as safety issue: No ]
  • Elucidation of metabolite structures and identification of major metabolites in plasma, urine, and faeces (if feasible) in comparison with various animal species (to be presented in a separate report) [ Time Frame: up to 336 h post treatment ] [ Designated as safety issue: No ]
  • Cblood cells/Cplasma ratio of 14C-radioactivity [ Time Frame: up to 168 h post treatment ] [ Designated as safety issue: No ]
  • concentrations of BI 671800 and its metabolite CD6384 in plasma and urine [ Time Frame: up to 336 h post treatment ] [ Designated as safety issue: No ]
  • concentrations of 14C-radioactivity in whole blood, plasma, urine, and faeces [ Time Frame: up to 336 h post treatment ] [ Designated as safety issue: No ]

Secondary Outcome Measures:
  • Changes from Baseline in Vital signs (pulse rate) [ Time Frame: up to 23 days post treatment ] [ Designated as safety issue: No ]
  • Changes from Baseline in Physical examination [ Time Frame: up to 23 days post treatment ] [ Designated as safety issue: No ]
  • Changes from Baseline in Vital signs (blood pressure) [ Time Frame: up to 23 days post treatment ] [ Designated as safety issue: No ]
  • Changes from Baseline in 12-lead electrocardiogram (ECG) [ Time Frame: up to 23 days post treatment ] [ Designated as safety issue: No ]
  • Changes from Baseline in Clinical laboratory tests [ Time Frame: up to 23 days post treatment ] [ Designated as safety issue: No ]
  • Occurrence of Adverse Events [ Time Frame: up to 23 days post treatment ] [ Designated as safety issue: No ]
  • Assessment of tolerability by investigator [ Time Frame: up to 23 days post treatment ] [ Designated as safety issue: No ]

Enrollment: 8
Study Start Date: September 2010
Primary Completion Date: October 2010 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: BI 671800 high dose
Oral drinking solution
Drug: BI 671800
High dose oral drinking solution

  Eligibility

Ages Eligible for Study:   18 Years to 55 Years
Genders Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion criteria:

  1. Healthy males according to a complete medical history, including the physical examination (to be performed at Day -1), vital signs (blood pressure, pulse rate), 12-lead Electrocardiogram (ECG), and clinical laboratory tests
  2. Age 18 to 55 years, inclusive
  3. Body mass index 18.0 to 30.0 kg/m2, inclusive
  4. Signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice (GCP) and the local legislation

Exclusion criteria:

  1. Any finding of the medical examination (including blood pressure, pulse rate, and ECG) deviating from normal and of clinical relevance
  2. Any evidence of a clinically relevant concomitant disease
  3. Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
  4. Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
  5. History of relevant orthostatic hypotension, fainting spells, or blackouts
  6. Chronic or relevant acute infections
  7. History of relevant allergy/hypersensitivity (including allergy to study drug or its excipients)
  8. Use of any prescription drugs 30 days prior to screening.
  9. Use of any over-the-counter, non-prescription preparations (including vitamins, minerals, and phytotherapeutic/herbal/plant-derived preparations) within 7 days prior to Check-in, unless deemed acceptable by the Investigator
  10. Participation in another trial with an investigational drug within 2 months prior to administration or during the trial
  11. Smoker (>10 cigarettes or >3 cigars or >3 pipes/day) or positive urine cotinine test at screening and check-in (Day -1)
  12. Inability to refrain from smoking during the stay in the trial centre
  13. Alcohol abuse (more than on average 2 units of alcoholic beverages per day or more than 14 units per week. One unit equals 1 pint (285 mL) of beer or lager, 1 glass (125 mL) of wine, or one shot (25 mL) of 40% spirit, or positive urine alcohol test at screening or check-in (Day -1)
  14. Drug abuse
  15. Blood donation (>100 mL within 60 days prior to study drug administration or during the trial)
  16. Excessive physical activity (within 1 week prior to administration or during the trial until follow-up examination)
  17. Any laboratory value outside the reference range that is of clinical relevance according to the investigator
  18. Inability to comply with dietary regimen of study centre
  19. A marked baseline prolongation of QT or QTc interval, history of additional risk factors for torsade de pointes (e.g. heart failure, hypokalaemia, family history of long QT syndrome)
  20. Veins unsuitable for blood sampling
  21. Exposure to diagnostic radiation for occupational reasons or during participation in a clinical trial in the previous year (except dental X-rays and plain X-rays of thorax and bony skeleton [excluding spinal column])
  22. Irregular defecation pattern (less than once per day)
  23. Unwillingness to use adequate contraception (condom plus another form of contraception e.g. spermicide, oral contraceptive taken by female partner, sterilisation, intrauterine device) during the entire study from the time of the first intake of study drug until 3 months after the last intake
  24. Any laboratory value outside the reference range that is of clinical relevance, especially repeated Alanine transaminase (ALT), Aspartate transaminase (AST), Gamma-glutamyltransferase (GGT), alkaline phosphatase, or total bilirubin above upper limit of normal at screening and not resolved before dosing
  25. Use of drugs which might reasonably influence the results of the trial or that prolong the QT/QTc interval within 10 days prior to administration or during the trial, and Cytochrome P-450 (CYP)2C8 substrates such as amiodarone, amodiaquine, paclitaxel, rosiglitazone, pioglitazone and repaglinide or CYP2C9 such as warfarin, tolbutamide, phenytoin, losartan, acenocoumarol within 1 month or six half lives (whichever is greater)
  Contacts and Locations
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Please refer to this study by its ClinicalTrials.gov identifier: NCT01205373

Locations
United States, Wisconsin
1268.7.001 Boehringer Ingelheim Investigational Site
Madison, Wisconsin, United States
Sponsors and Collaborators
Boehringer Ingelheim
Investigators
Study Chair: Boehringer Ingelheim Boehringer Ingelheim
  More Information

No publications provided

Responsible Party: Boehringer Ingelheim, Study Chair, Boehringer Ingelheim
ClinicalTrials.gov Identifier: NCT01205373     History of Changes
Other Study ID Numbers: 1268.7, 2009-016370-32
Study First Received: September 17, 2010
Last Updated: October 31, 2013
Health Authority: United States: Food and Drug Administration

Additional relevant MeSH terms:
Pharmaceutical Solutions
Therapeutic Uses
Pharmacologic Actions

ClinicalTrials.gov processed this record on September 11, 2014