Metabolism and Pharmacokinetics of [14C]-BI 409306 After Administration as Oral Solution in Healthy Male Volunteers

NCT02597998 | Completed Phase 1 Results

• 2 other identifiers: 1289.262015-001877-42
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

The aim of this study is to assess the mass balance recovery from excreta of carbon 14 labelled BI409306 (\[14C\] BI 409306) in healthy, CYP2C19 genotyped subjects and to provide plasma, urine and faecal samples for metabolite profiling and structural identification.

Conditions

Healthy

Outcome Measures

Primary Outcomes (1)

• Mass Balance Recovery of Total Radioactivity in Urine and Faeces: Amount Excreted Within the Time Interval From 0 to the Time of the Last Quantifiable Data Point as a Percentage of the Administered Dose (fe0-tz) for Urine and Faeces

  Mass balance recovery of total radioactivity in urine and faeces: Amount excreted within the time interval from 0 to the time of the last quantifiable data point as a percentage of the administered dose (fe0-tz) for urine and faeces. Urine collection intervals: -17:00-0:00 hours before drug administration and, 0-4, 4-8, 8-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192 and 192-216 hours after drug administration. Faeces collection intervals: -17:00-0:00, 0-24, 24-48, 48-72, 72-96, 96- 20, 120-144, 144-168, 168-192 and 192-216 hours after drug administration.

  Urine and faeces sample collection: 17 hours before and up to 216 hours after drug administration. The details are mentioned in description section.

Secondary Outcomes (4)

• Maximum Measured Concentration of BI 409306 in Plasma (Cmax)

  PK plasma samples were taken at: 2:00 (hour: minute) before drug administration and 0:10, 0:20, 0:30, 0:45, 1, 1:30, 2, 2:30, 3, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, 144, 168 hours after drug administration.

• Maximum Measured Concentration of 14C-BI 409306 Related Radioactivity in Plasma (Cmax)

  PK plasma samples were taken at: 2:00 (hour: minute) before drug administration and 0:10, 0:20, 0:30, 0:45, 1, 1:30, 2, 2:30, 3, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, 144, 168 hours after drug administration.

• Area Under the Concentration-time Curve Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) for BI 409306 in Plasma

  PK plasma samples were taken at: 2:00 (hour: minute) before drug administration and 0:10, 0:20, 0:30, 0:45, 1, 1:30, 2, 2:30, 3, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, 144, 168 hours after drug administration.

• Area Under the Concentration-time Curve Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) for 14C-BI 409306 Related Radioactivity in Plasma

  PK plasma samples were taken at: 2:00 (hour: minute) before drug administration and 0:10, 0:20, 0:30, 0:45, 1, 1:30, 2, 2:30, 3, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, 144, 168 hours after drug administration.

Study Arms (1)

14C-BI 409306 - 25 mg

EXPERIMENTAL

14C-BI 409306 oral solution

Drug: 14C-BI 409306

Interventions

14C-BI 409306 DRUG

Also known as: 14C-BI 409306 oral solution

14C-BI 409306 - 25 mg

Eligibility Criteria

• Age: 30 Years - 65 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Healthy male genotyped as CY2C19 poor metabolizer (PM) or extensive metabolizer (EM) according to the investigator's assessment, based on a complete medical history including a physical examination, vital signs (BP - Blood Pressure, PR - Pulse Rate), 12-lead ECG (Electrogardiogramm), and clinical laboratory tests. PM is defined as carrier of two non-functional alleles \*2 and \*3 of the CYP2C19 gene (diplotypes \*2/\*2; \*2/\*3; \*3/\*3). EM is defined as carrier of two functional alleles of the CYP2C19 gene (absence of \*2, \*3, \*17; diplotype \*1/\*1).
• Age of 30 to 65 years (incl.).
• BMI (Body Mass Index) of 18.5 to 29.9 kg/m2 (incl.).
• Signed and dated written informed consent prior to admission to the study in accordance with GCP and local legislation.
• A history of regular bowel movements (averaging 1 or more bowel movements per day; subjects with regular bowel movements of \>3 per day will be excluded).
• Subjects who are sexually active must use, with their partner, 2 approved methods of highly effective contraception from the time of IMP administration until 90 days after the last dose of IMP.

You may not qualify if:

• Any finding in the medical examination (including BP - Blood Pressure, PR - Pulse Rate or ECG - Electrocardiogramm) is deviating from normal and judged as clinically relevant by the investigator
• Repeated measurement of systolic blood pressure outside the range of 90 to 140 mmHg, diastolic blood pressure outside the range of 50 to 90 mmHg, or pulse rate outside the range of 45 to 90 bpm
• Any laboratory value outside the reference range that the investigator considers to be of clinical relevance
• Any evidence of a concomitant disease judged as clinically relevant by the investigator
• Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders. Any significant history of ocular or eye disease.
• Surgery of the gastrointestinal tract that could interfere with kinetics of the trial medication (except appendectomy and simple hernia repair)
• Diseases of the central nervous system (including but not limited to any kind of seizures or stroke), and other relevant neurological or psychiatric disorders

Sponsors & Collaborators

• Boehringer Ingelheim: lead

Study Sites (1)

Quotient Sciences

Nottingham, NG11 6JS, United Kingdom

Location

Related Links

• Related Info

Results Point of Contact

• Title: Boehringer Ingelheim, Call Center
• Organization: Boehringer Ingelheim

clintriage.rdg@boehringer-ingelheim.com

1-800-243-0127

Study Officials

• Boehringer Ingelheim

  Boehringer Ingelheim

  STUDY CHAIR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: OTHER
• Restrictive Agreement: Yes

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: September 30, 2015
• First Posted: November 5, 2015
• Study Start: September 15, 2015
• Primary Completion: December 11, 2015
• Study Completion: December 11, 2015
• Last Updated: March 7, 2024
• Results First Posted: March 7, 2024

Record last verified: 2023-08

Data Sharing

• IPD Sharing: Will not share

Locations

GB (1)