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Metabolism and Pharmacokinetics of [14C]-BI 44370 BS Administered as an Oral Solution in Healthy Male Volunteers

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ClinicalTrials.gov Identifier: NCT02215772
Recruitment Status : Completed
First Posted : August 13, 2014
Last Update Posted : August 13, 2014
Sponsor:
Information provided by (Responsible Party):
Boehringer Ingelheim

Brief Summary:
Study to investigate the basic pharmacokinetics of BI 44370 BS, its metabolite CD 10419 BS, and 14C-radioactivity including mass balance, excretion pathways, and metabolism following a single oral administration of 200 mg [14C]BI 44370 BS to healthy male volunteers and to evaluate safety and tolerability following a single oral administration of 200 mg [14C]BI 44370 BS to healthy male volunteers

Condition or disease Intervention/treatment Phase
Healthy Drug: BI 44370 BS Phase 1

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Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 8 participants
Intervention Model: Single Group Assignment
Masking: None (Open Label)
Primary Purpose: Treatment
Official Title: A Phase I Trial to Investigate the Metabolism and Pharmacokinetics of an Open Label Single Dose of 200 mg [14C]-BI 44370 BS Administered as an Oral Solution in Healthy Male Volunteers
Study Start Date : September 2008
Actual Primary Completion Date : October 2008

Arm Intervention/treatment
Experimental: BI 44370 BS
200 mg containing 2.43 megabecquerel (MBq) 14C-radioactivity
Drug: BI 44370 BS



Primary Outcome Measures :
  1. Individual time course profiles of [14C]-radioactivity in whole blood, plasma, urine [ Time Frame: up to day 15 ]
    in nmoleq/L

  2. Individual time course profiles of [14C]-radioactivity in faeces [ Time Frame: up to day 15 ]
    in nmoleq/kg

  3. Individual time course profiles of BI 44370 BS (and its glucuronide CD 10419 BS) in plasma and urine [ Time Frame: up to 15 days ]
  4. Rate and extent of excretion mass balance based on the total radioactivity in urine and faeces [ Time Frame: up to 15 days ]
  5. Cblood cells/Cplasma ratio of [14C]-radioactivity [ Time Frame: up to 12 hours after drug administration ]
  6. Cblood /Cplasma ratio of [14C]-radioactivity [ Time Frame: up to 144 hours after drug administration ]
  7. Identification of major metabolites in plasma, urine, and faeces [ Time Frame: up to day 15 ]
  8. Cmax (maximum concentration of the analyte(s) in plasma) [ Time Frame: up to 144 hours after drug administration ]
  9. tmax (time from dosing to the maximum concentration of the analyte(s) in plasma) [ Time Frame: up to 144 hours after drug administration ]
  10. AUC0-tz (area under the concentration-time curve of the analyte(s) in plasma over the time interval from 0 to the time of the last quantifiable data point) [ Time Frame: up to 144 hours after drug administration ]
  11. AUC0-inf. (area under the concentration-time curve of the analyte(s) in plasma over the time interval from 0 to infinity) [ Time Frame: up to 144 hours after drug administration ]
  12. λz (terminal rate constant in plasma) [ Time Frame: up to 144 hours after drug administration ]
  13. t1/2 (terminal half-life of the analyte(s) in plasma) [ Time Frame: up to 144 hours after drug administration ]
  14. MRTpo (mean residence time of the analyte(s) in the body after oral administration) [ Time Frame: up to 144 hours after drug administration ]
  15. CL/F (total clearance of the analyte in plasma after oral administration) [ Time Frame: up to 144 hours after drug administration ]
  16. Vz/F (apparent volume of distribution during the terminal phase λz following an oral dose) [ Time Frame: up to 144 hours after drug administration ]
  17. Ae0-tz (amount of analyte that is eliminated in urine within the time interval zero to tz, additionally excretion within each sampling interval will be calculated) [ Time Frame: up to 15 days ]
  18. fe0-tz (fraction of analyte excreted in urine within the time interval zero to tz in % of dose, additionally excretion within each sampling interval will be calculated) [ Time Frame: up to 15 days ]
  19. Aefaeces,0-tz (amount of analyte excreted in faeces within the time interval zero to tz, additionally excretion within each sampling interval will be calculated) [ Time Frame: up to 15 days ]
  20. fefaeces,0-tz (fraction of analyte excreted in faeces within the time interval zero to tz in % of dose, additionally excretion within each sampling interval will be calculated) [ Time Frame: up to 15 days ]
  21. CLR,t1-t2 (renal clearance of analyte from the within the time interval t1 to t2) [ Time Frame: up to 15 days ]

Secondary Outcome Measures :
  1. Number of patients with clinically relevant findings in vital signs [ Time Frame: up to 23 days ]
  2. Number of patients with clinically relevant findings in 12-lead electrocardiogram (ECG) [ Time Frame: up to 23 days ]
  3. Number of patients with clinically relevant laboratory findings [ Time Frame: up to 23 days ]
  4. Number of patients with adverse events [ Time Frame: up to up to 44 days ]
  5. Assessment of global tolerability on a 4-point scale [ Time Frame: day 15 ]


Information from the National Library of Medicine

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Ages Eligible for Study:   18 Years to 65 Years   (Adult, Older Adult)
Sexes Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria:

  • Healthy males according to the following criteria based upon a complete medical history, including the physical examination, vital signs (blood pressure (BP), pulse rate (PR)), 12-lead ECG, clinical laboratory tests
  • Age ≥18 and ≤65 years
  • Body mass index (BMI) ≥18.0 and BMI ≤30.0 kg/m2
  • 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:

  • Any finding of the medical examination (including BP, PR and ECG) deviating from normal and of clinical relevance
  • Any evidence of a clinically relevant concomitant disease
  • 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 relevant orthostatic hypotension, fainting spells or blackouts
  • Chronic, or relevant acute infections
  • History of relevant allergy/hypersensitivity (including allergy to study drug or its excipients)
  • Intake of drugs with a long half-life (> 24 hours) within at least one month or less than 10 half-lives of the respective drug prior to administration or during the trial
  • Use of drugs which might reasonably influence the results of the trial based on the knowledge at the time of protocol preparation within 10 days prior to administration until after the last sample from Visit 2 is collected
  • Participation in another trial with an investigational drug within two months prior to administration or during the trial
  • Smoker (> 10 cigarettes or > 3 cigars or > 3 pipes/day)
  • Inability to refrain from smoking during the stay in the trial centre
  • Alcohol abuse (more than on average 2 units of alcoholic beverages per day or more than 14 units per week (1 unit equals 1 pint [285 mL] of beer or lager, 1 glass [125 mL] of wine, 25 mL shot of 40% spirit))
  • Drug abuse
  • Blood donation (more than 100 mL within 60 days prior to study drug administration or during the trial)
  • Excessive physical activities (within one week prior to administration or during the trial until follow-up examination)
  • Any laboratory value outside the reference range that is of clinical relevance
  • Inability to comply with dietary regimen of study centre
  • A marked baseline prolongation of QT/QTc interval (e.g., repeated demonstration of a QTc interval >450 ms)
  • Veins unsuitable for blood sampling
  • PR interval >220 ms or QRS interval >120 ms
  • Exposure to radiation for diagnostic reasons (except dental X-rays and plain X-rays of thorax and bony skeleton (excluding spinal column)), during work or during participation in a medical trial in the previous year
  • Irregular defecation pattern (less than once per 2 days)
  • Not willing to use adequate contraception (condoms use plus another form of contraception e.g. spermicide, oral contraceptive taken by female partner, sterilisation, intrauterine device) during the whole study period from the time of the first intake of study drug until three months after the last intake

Additional Information:
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Responsible Party: Boehringer Ingelheim
ClinicalTrials.gov Identifier: NCT02215772    
Other Study ID Numbers: 1246.14
First Posted: August 13, 2014    Key Record Dates
Last Update Posted: August 13, 2014
Last Verified: August 2014