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

NCT02215772 | Completed Phase 1

• 1 other identifier: 1246.14
• Study Type: interventional
• Target: 8
• Locations: 0 countries
• Sites: N/A

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

Conditions

Healthy

Outcome Measures

Primary Outcomes (21)

• Individual time course profiles of [14C]-radioactivity in whole blood, plasma, urine

  in nmoleq/L

  up to day 15

• Individual time course profiles of [14C]-radioactivity in faeces

  in nmoleq/kg

  up to day 15

• Individual time course profiles of BI 44370 BS (and its glucuronide CD 10419 BS) in plasma and urine

  up to 15 days

• Rate and extent of excretion mass balance based on the total radioactivity in urine and faeces

  up to 15 days

• Cblood cells/Cplasma ratio of [14C]-radioactivity

  up to 12 hours after drug administration

• Cblood /Cplasma ratio of [14C]-radioactivity

  up to 144 hours after drug administration

• Identification of major metabolites in plasma, urine, and faeces

  up to day 15

• Cmax (maximum concentration of the analyte(s) in plasma)

  up to 144 hours after drug administration

• tmax (time from dosing to the maximum concentration of the analyte(s) in plasma)

  up to 144 hours after drug administration

• 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)

  up to 144 hours after drug administration

• AUC0-inf. (area under the concentration-time curve of the analyte(s) in plasma over the time interval from 0 to infinity)

  up to 144 hours after drug administration

• λz (terminal rate constant in plasma)

  up to 144 hours after drug administration

• t1/2 (terminal half-life of the analyte(s) in plasma)

  up to 144 hours after drug administration

• MRTpo (mean residence time of the analyte(s) in the body after oral administration)

  up to 144 hours after drug administration

• CL/F (total clearance of the analyte in plasma after oral administration)

  up to 144 hours after drug administration

• Vz/F (apparent volume of distribution during the terminal phase λz following an oral dose)

  up to 144 hours after drug administration

• 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)

  up to 15 days

• 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)

  up to 15 days

• 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)

  up to 15 days

• 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)

  up to 15 days

• CLR,t1-t2 (renal clearance of analyte from the within the time interval t1 to t2)

  up to 15 days

Secondary Outcomes (5)

• Number of patients with clinically relevant findings in vital signs

  up to 23 days

• Number of patients with clinically relevant findings in 12-lead electrocardiogram (ECG)

  up to 23 days

• Number of patients with clinically relevant laboratory findings

  up to 23 days

• Number of patients with adverse events

  up to up to 44 days

• Assessment of global tolerability on a 4-point scale

  day 15

Study Arms (1)

BI 44370 BS

EXPERIMENTAL

200 mg containing 2.43 megabecquerel (MBq) 14C-radioactivity

Drug: BI 44370 BS

Interventions

BI 44370 BS DRUG

BI 44370 BS

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• 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

You may not qualify if:

• 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)

Sponsors & Collaborators

• Boehringer Ingelheim: lead

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: August 12, 2014
• First Posted: August 13, 2014
• Study Start: September 1, 2008
• Primary Completion: October 1, 2008
• Last Updated: August 13, 2014

Record last verified: 2014-08