Metabolism and Pharmacokinetics of [14C] BEA 2180 BR Administered Orally Compared to [14C] BEA 2180 BR Administered Intravenously in Healthy Male Volunteers

NCT02258971 | Completed Phase 1

• 1 other identifier: 1205.8
• Study Type: interventional
• Target: 14
• Locations: 0 countries
• Sites: N/A

Brief Summary

Primary objectives: To determine the basic pharmacokinetics of BEA 2180 BR, its metabolites CD 1975 ZW and CD 1976 ZW and radioactivity including excretion mass balance, excretion pathways and metabolism following the oral and intravenous administration of \[14C\] BEA 2180 BR Secondary objectives: To determine safety and tolerability following single dose oral and iv administration of BEA 2180 BR in healthy male volunteers.

Conditions

Healthy

Outcome Measures

Primary Outcomes (19)

• Individual time course profiles of [14C] radioactivity

  Up to 312 hours after drug administration

• Individual time course profiles of BEA 2180 and its metabolites CD 1975 ZW and CD 1976 ZW

  Up to 312 hours after drug administration

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

  Up to 312 hours after drug administration

• Elucidation of metabolite structures and identification of major metabolites in plasma, urine, and faeces (if feasible) in comparison with various animal species

  Up to 312 hours after drug administration

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

  Up to 96 hours after drug administration

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

  Up to 96 hours after drug administration

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

  Up to 96 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 96 hours after drug administration

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

  Up to 96 hours after drug administration

• λz (terminal rate constant in plasma)

  Up to 96 hours after drug administration

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

  Up to 96 hours after drug administration

• MRT (mean residence time of the analyte(s) in the body)

  Up to 96 hours after drug administration

• CL (total clearance of the analyte in plasma)

  Up to 96 hours after drug administration

• Vz (apparent volume of distribution during the terminal phase λz)

  Up to 96 hours after drug administration

• Vss (apparent volume of distribution at steady state)

  Up to 96 hours after drug administration

• fe0-tz (amount of analyte excreted in urine within the time interval zero to tz in % of dose)

  Up to 312 hours after drug administration

• fefaeces,0-tz (amount 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 312 hours after drug administration

• CLR,0-tz (renal clearance of analyte)

  Up to 96 hours after drug administration

• Fa (fraction of drug absorbed after oral administration based on radioactivity data) based on oral and i.v. data

  Up to 96 hours after drug administration

Secondary Outcomes (7)

• Number of participants with abnormal findings in physical examination

  Up to day 29 after first drug administration

• Number of participants with clinically significant changes in vital signs

  Up to day 29 after first drug administration

• Number of participants with abnormal findings in 12-lead ECG

  Up to day 29 after first drug administration

• Number of participants with abnormal changes in clinical laboratory parameters

  Up to day 29 after first drug administration

• Number of participants with adverse events

  Up to day 29 after first drug administration

Study Arms (2)

BEA 2180 BR oral

EXPERIMENTAL

Drug: BEA 2180 BR oral

BEA 2180 BR infusion

ACTIVE COMPARATOR

Drug: BEA 2180 BR infusion

Interventions

BEA 2180 BR oral DRUG

Oral solution

BEA 2180 BR oral

BEA 2180 BR infusion DRUG

Solution for infusion to be reconstituted with isotonic saline

BEA 2180 BR infusion

Eligibility Criteria

• Age: 35 Years - 70 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 (BP, PR), 12-lead electrocardiogram (ECG), clinical laboratory tests
• Age ≥35 and Age ≤70 years
• BMI ≥18.5 and BMI ≤29.9 kg/m2 (Body Mass Index)
• Subjects must agree to minimize the risk of female partners becoming pregnant from the dosing day until 3 months after the completion of the study. Acceptable methods of contraception for male volunteers include a vasectomy no less than 3 months prior to dosing, barrier contraception or a medically accepted contraceptive method. For female partners of male volunteers, acceptable methods of contraception include intra-uterine device, tubal ligation, hormonal contraceptive since at least two months and diaphragm with spermicide
• 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 blood pressure (BP), pulse rate (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 or during the trial
• 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 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)more than 60 g/day).
• 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: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: October 1, 2014
• First Posted: October 8, 2014
• Study Start: March 1, 2007
• Primary Completion: May 1, 2007
• Last Updated: October 8, 2014

Record last verified: 2014-09