A Study in Healthy Men to Test How BI 1265162 is Taken up and Processed by the Body

NCT04267276 | Terminated Phase 1 Results

• 2 other identifiers: 1399-00132019-003389-42
• Study Type: interventional
• Target: 7
• Locations: 1 country
• Sites: 1

Brief Summary

To investigate rates and routes of excretion, mass balance, pharmacokinetics of parent drug, any known metabolites, and total radioactivity, metabolite profiling, metabolite identification, if suitable assays are available, safety and tolerability in healthy male subjects.

Conditions

Healthy Volunteers

Outcome Measures

Primary Outcomes (2)

• Part 1: Mass Balance Recovery of Total (C-14) BI 1265162-radioactivity in Urine

  Mass balance recovery assessed as amount of (C-14) BI 1265162-radioactivity excreted as a percentage of the single intravenous administered dose of BI 1265162 (C-14) over the time interval from 0 to 192 hours. The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis.

  On Day -1 or Day 1 pre-dose (blank) sample, on Day 1 prior to start of urine collection voiding of the bladder, 0-4 , 4-8, 8-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, and 168-192 hours after administration of BI 1265162 (C-14).

• Part 1: Mass Balance Recovery of Total (C-14) BI 1265162-radioactivity in Faeces.

  Mass balance recovery assessed as amount of (C-14) BI 1265162-radioactivity excreted as a percentage of the single intravenous administered dose of BI 1265162 (C-14) over the time interval from 0 to 192 hours. The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis.

  On Day -2, Day -1 or Day 1 pre-dose (blank) sample, and on Day 1 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, and 168-192 hours after administration of BI 1265162 (C-14).

Secondary Outcomes (7)

• Part 1: Area Under the Concentration-time Curve of Total [14C]BI 1265162-equivalent (EQ) in Plasma Over the Time Interval From 0 to 192 Hours (the Last Quantifiable Data Point (AUC0-tz))

  At 02:00 hours:minutes pre-dose and at 0:05, 00:30, 00:59 01:05, 01:10, 01:40, 02:00, 03:00, 04:00, 05:00, 07:00, 08:00, 09:00, 11:00, 12:00, 24:00, 48:00, 72:00, 96:00, 120:00, 144:00, 168:00, 192:00 after single dose of BI 1265162 (C-14).

• Part 1: Area Under the Concentration-time Curve of Total BI 1265162 in Plasma Over the Time Interval From 0 to 192 Hours (the Last Quantifiable Data Point (AUC0-tz))

  At 02:00 hours:minutes pre-dose and at 0:05, 00:30, 00:59 01:05, 01:10, 01:40, 02:00, 03:00, 04:00, 05:00, 07:00, 08:00, 09:00, 11:00, 12:00, 24:00, 48:00, 72:00, 96:00, 120:00, 144:00, 168:00, 192:00 after single dose of BI 1265162 (C-14).

• Part 1: Area Under the Concentration-time Curve of Total BI 1265162 Metabolite M582 in Plasma Over the Time Interval From 0 to 192 Hours (the Last Quantifiable Data Point (AUC0-tz))

  At 02:00 hours:minutes pre-dose and at 0:05, 00:30, 00:59 01:05, 01:10, 01:40, 02:00, 03:00, 04:00, 05:00, 07:00, 08:00, 09:00, 11:00, 12:00, 24:00, 48:00, 72:00, 96:00, 120:00, 144:00, 168:00, 192:00 after single dose of BI 1265162 (C-14).

• Part 1: Maximum Measured Concentration (Cmax) of Total [14C]BI 1265162-equivalent (EQ) in Plasma

  At 02:00 hours:minutes pre-dose and at 0:05, 00:30, 00:59 01:05, 01:10, 01:40, 02:00, 03:00, 04:00, 05:00, 07:00, 08:00, 09:00, 11:00, 12:00, 24:00, 48:00, 72:00, 96:00, 120:00, 144:00, 168:00, 192:00 after single dose of BI 1265162 (C-14).

• Part 1: Maximum Measured Concentration (Cmax) of Total BI 1265162 in Plasma

  At 02:00 hours:minutes pre-dose and at 0:05, 00:30, 00:59 01:05, 01:10, 01:40, 02:00, 03:00, 04:00, 05:00, 07:00, 08:00, 09:00, 11:00, 12:00, 24:00, 48:00, 72:00, 96:00, 120:00, 144:00, 168:00, 192:00 after single dose of BI 1265162 (C-14).

Study Arms (2)

Part 1: BI 1265162 - intravenous

EXPERIMENTAL

Drug: Part 1: BI 1265162 - intravenous

Part 2: BI 1265162 - oral

EXPERIMENTAL

Drug: Part 2: BI 1265162 - oral

Interventions

Part 1: BI 1265162 - intravenous DRUG

Intravenous solution

Part 1: BI 1265162 - intravenous

Part 2: BI 1265162 - oral DRUG

Oral solution

Part 2: BI 1265162 - oral

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 male subjects according to the assessment of the investigator, as based on a complete medical history including a physical examination, vital signs (blood pressure (BP), pulse rate (PR)), 12-lead electrocrdiogram (ECG), and clinical laboratory tests
• Age of 18 to 65 years (inclusive)
• Body mass index (BMI) of 18.5 to 29.9 kg/m2 (inclusive)
• Signed and dated written informed consent prior to admission to the trial, in accordance with Good Clinical Practice (GCP) and local legislation
• Subjects who are sexually active must use, with their partner, highly effective contraception from the time of administration of trial medication until 3 months after administration of trial medication. Adequate methods are:
• Condoms plus use of hormonal contraception by the female partner that started at least 2 months prior to administration of trial medication (e.g., implants, injectables, combined oral or vaginal contraceptives, intrauterine device), or
• Condoms plus surgical sterilization (vasectomy at least 1 year prior to enrolment), or
• Condoms plus surgically sterilised partner (including hysterectomy), or
• Condoms plus intrauterine device, or
• Condoms plus partner of non-child bearing potential (including homosexual men) Subjects are required to use condoms to prevent unintended exposure of the partner to the trial drug via seminal fluid.
• Alternatively, true abstinence is acceptable when it is in line with the subject's preferred and usual lifestyle. If a subject is usually not sexually active but becomes active, with their partner, they must comply with the contraceptive requirements detailed above.

You may not qualify if:

• Any finding in the medical examination (including BP, PR or ECG) deviating from normal and assessed as clinically relevant by the investigator
• Repeated measurement of systolic blood pressure outside the range of 90 to 139 mmHg, diastolic blood pressure outside the range of 45 to 89 mmHg, or pulse rate outside the range of 40 to 100 bpm
• Any laboratory value outside the reference range that the investigator considers to be of clinical relevance
• Any evidence of a concomitant disease assessed as clinically relevant by the investigator
• Clinically significant gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
• Cholecystectomy or other surgery of the gastrointestinal tract that could interfere with the pharmacokinetics of the trial medication (except appendectomy or 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
• History of relevant orthostatic hypotension, fainting spells, or blackouts
• Chronic or relevant acute infections
• History of relevant allergy or hypersensitivity (including allergy to the trial medication or its excipients)
• Use of drugs within 30 days of planned administration of trial medication that might reasonably influence the results of the trial (including drugs that cause QT/ QTc interval prolongation)
• Intake of an investigational drug in another clinical trial within 60 days of planned administration of investigational drug in the current trial, or concurrent participation in another clinical trial in which investigational drug is administered
• Smoking habit other than incidental. Incidental smoker is defined as a person who will not smoke more than 5 cigarettes per week
• Inability to refrain from smoking in the clinical research unit
• Alcohol abuse (average intake of more than 24 units of alcohol per week (1 unit of alcohol equals approximately 250 mL of beer, 100 mL of wine or 35 mL of spirits))

Sponsors & Collaborators

• Boehringer Ingelheim: lead

Study Sites (1)

PRA Health Sciences Onderzoekscentrum Martini

Groningen, 9728 NZ, Netherlands

Location

Related Links

• Related Info

Limitations and Caveats

The study was interrupted due to COVID-19 crisis on 02-Apr-2020, after completion of Part 1. Further, the sponsor decided to discontinue the development of BI 1265162. Enrolment in Part 2 (oral administration of BI 1265162 (C-14)) did not take place. Decision to terminate trial was taken on 17-Dec-2020.

Results Point of Contact

• Title: Boehringer Ingelheim
• Organization: Boehringer Ingelheim

clintriage.rdg@boehringer-ingelheim.com

1-800-243-0127

Publication Agreements

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

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: February 11, 2020
• First Posted: February 12, 2020
• Study Start: February 18, 2020
• Primary Completion: April 2, 2020
• Study Completion: April 2, 2020
• Last Updated: June 1, 2022
• Results First Posted: February 23, 2022

Record last verified: 2022-05

Data Sharing

• IPD Sharing: Will not share

Locations

NL (1)