Safety, Pharmacokinetics, and Pharmacodynamics of BIRT 2584 XX Administered as Multiple Doses and Safety and Pharmacokinetics of BIRT 2584 XX Administered With and Without Food as Single Dose to Healthy Male Volunteers

October 2, 2014 updated by: Boehringer Ingelheim

Safety, Pharmacokinetics, and Pharmacodynamics of BIRT 2584 XX Administered as Multiple Doses of 100 mg to 750 mg qd for 14 or 28 Days (Randomised, Double-blind Placebo Controlled Design), and Safety and Pharmacokinetics of 500 mg of BIRT 2584 XX Administered With and Without Food as Single Dose (Open, Intra-individual Comparison) to Healthy Male Volunteers

The study comprised two parts. The objective of the first study period was to assess the safety and pharmacokinetics of 500 mg of BIRT 2584 XX tablets administered with and without food in male healthy volunteers and to determine the relative bioavailability of the BIRT 2584 XX tablet formulation compared by historical comparison to BIRT 2584 XX powder in PEG 400 (U05-2074) (part 1). The second and major phase of the trial was aimed at evaluating the safety, tolerability, pharmacokinetics, and pharmacodynamics of multiple rising doses of BIRT 2584 XX (100 mg, 250 mg, and 500 mg bid on the first 2 days and qd on the following 12 days, or 750 mg qd for 28 days) in healthy male subjects (part 2)

Study Overview

Status

Status

Indicates the current recruitment status or the expanded access status.
Completed

Conditions

Conditions

The disease, disorder, syndrome, illness, or injury that is being studied. On ClinicalTrials.gov, conditions may also include other health-related issues, such as lifespan, quality of life, and health risks.

Intervention / Treatment

Intervention / Treatment

A process or action that is the focus of a clinical study. Interventions include drugs, medical devices, procedures, vaccines, and other products that are either investigational or already available. Interventions can also include noninvasive approaches, such as education or modifying diet and exercise.

Study Type

Study Type

Describes the nature of a clinical study. Study types include interventional studies (also called clinical trials), observational studies (including patient registries), and expanded access.
Interventional

Enrollment (Actual)

Enrollment

The number of participants in a clinical study. The "anticipated" enrollment is the target number of participants that the researchers need for the study.
74

Phase

Phase

The stage of a clinical trial studying a drug or biological product, based on definitions developed by the U.S. Food and Drug Administration (FDA). The phase is based on the study's objective, the number of participants, and other characteristics. There are five phases: Early Phase 1 (formerly listed as Phase 0), Phase 1, Phase 2, Phase 3, and Phase 4. Not Applicable is used to describe trials without FDA-defined phases, including trials of devices or behavioral interventions.
  • Phase 1

Participation Criteria

Researchers look for people who fit a certain description, called eligibility criteria. Some examples of these criteria are a person's general health condition or prior treatments.

Eligibility Criteria

Eligibility Criteria

The key requirements that people who want to participate in a clinical study must meet or the characteristics they must have. Eligibility criteria consist of both inclusion criteria (which are required for a person to participate in the study) and exclusion criteria (which prevent a person from participating). Types of eligibility criteria include whether a study accepts healthy volunteers, has age or age group requirements, or is limited by sex.

Ages Eligible for Study

18 years to 63 years (Adult)

Accepts Healthy Volunteers

Yes

Genders Eligible for Study

Male

Description

Inclusion Criteria:

  • Healthy male subjects as determined by results of the screening
  • Signed written informed consent in accordance with Good Clinical Practice (GCP) and local legislation
  • Age ≥ 18 and ≤ 63 years
  • BMI ≥ 18.5 and ≤ 29.9 kg/m2

Exclusion Criteria:

  • Any finding during the medical examination (including blood pressure, pulse rate, and electrocardiogram) deviating from normal and of clinical relevance
  • Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hematological, oncological, or hormonal disorders
  • Surgery of gastrointestinal tract (except appendectomy)
  • Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
  • Relevant history of orthostatic hypotension, fainting spells, or blackouts
  • Chronic or relevant acute infections
  • History of allergy/hypersensitivity (including drug allergy) considered relevant to the trial as judged by the investigator
  • Intake of drugs with a long half-life (greater than 24 hours) (less than 1 month prior to administration or during the trial)
  • Use of any drugs, which might influence the results of the trial (less than 10 days prior to study drug administration or expected during the trial)
  • Participation in another trial with an investigational drug (less than 2 months prior to administration or expected during trial)
  • Smoker (more than 10 cigarettes/day or more than 3 cigars/day or more than 3 pipes/day)
  • Alcohol abuse (more than 60 g of ethanol per day)
  • Drug abuse
  • Blood donation or loss greater than 400 mL (less than 1 month prior to administration or expected during the trial)
  • Clinically relevant laboratory abnormalities

Study Plan

This section provides details of the study plan, including how the study is designed and what the study is measuring.

How is the study designed?

Design Details

  • Primary Purpose: Treatment
  • Allocation: Randomized
  • Interventional Model: Parallel Assignment
  • Masking: Double

Arms and Interventions

Participant Group / Arm

Participant Group / Arm

A group or subgroup of participants in a clinical trial that receives a specific intervention/treatment, or no intervention, according to the trial's protocol.
Intervention / Treatment

Intervention / Treatment

A process or action that is the focus of a clinical study. Interventions include drugs, medical devices, procedures, vaccines, and other products that are either investigational or already available. Interventions can also include noninvasive approaches, such as education or modifying diet and exercise.
Experimental: BIRT 2584 XX - single dose

Part 1 - bioavailability/food effect

two single doses, 30 minutes prior to the second drug administration after a one week wash-out period, a standardised high fat, high caloric meal was served
Drug: BIRT 2584 XX - single dose
Other: high caloric meal
30 minutes prior to the second drug administration after a one week wash-out period, a standardised high fat, high caloric meal was served
Placebo Comparator: Placebo
Part 2
Drug: Placebo
Experimental: BIRT 2584 XX - multiple escalating dose
Part 2 - multiple escalating dose, 14 days and 28 days
Drug: BIRT 2584 XX - multiple escalating dose

What is the study measuring?

Primary Outcome Measures

Primary Outcome Measures

In a clinical study's protocol, the planned outcome measure that is the most important for evaluating the effect of an intervention/treatment. Most clinical studies have one primary outcome measure, but some have more than one.
Outcome Measure
Measure Description
Time Frame
Number of subjects with abnormal findings in physical examination
Time Frame: up to 45 days
up to 45 days
Number of subjects with abnormal changes in laboratory parameters
Time Frame: up to 45 days
up to 45 days
Number of subjects with clinically significant changes in vital signs
Time Frame: up to 45 days
Pulse rate, systolic, and diastolic blood pressure
up to 45 days
Number of subjects with adverse events
Time Frame: up to 59 days
up to 59 days
Number of subjects with clinically significant changes in 12-lead ECG
Time Frame: up to 45 days
up to 45 days

Secondary Outcome Measures

Secondary Outcome Measures

In a clinical study's protocol, a planned outcome measure that is not as important as the primary outcome measure for evaluating the effect of an intervention but is still of interest. Most clinical studies have more than one secondary outcome measure.
Outcome Measure
Measure Description
Time Frame
AUC0-inf (area under the concentration-time curve of BIRT 2584 XX in plasma over the time interval from 0 to infinity)
Time Frame: up to 72 hours
bioavailability/food effect part
up to 72 hours
Cmax (maximum concentration of BIRT 2584 XX in plasma)
Time Frame: up to 72 hours
bioavailability/food effect part
up to 72 hours
tmax (time from dosing to maximum concentration of BIRT 2584 XX and BI 610100, its major metabolite in humans)
Time Frame: up to 72 hours
bioavailability/food effect part
up to 72 hours
Cmax (maximum concentration of BIRT 2584 XX and BI 610100 in plasma)
Time Frame: up to 42 days
multiple rising dose part
up to 42 days
tmax (time from dosing to maximum concentration of BIRT 2584 XX and BI 610100)
Time Frame: up to 42 days
multiple rising dose part
up to 42 days
AUC0-12 (area under the concentration-time curve of BIRT 2584 XX and BI 610100 in plasma over the time interval from 0 to 12 hours after the first dose
Time Frame: up to 14 hours after first drug administration
multiple rising dose part
up to 14 hours after first drug administration
AUCtau,l (area under the concentration-time curve of BIRT 2584 XX and BI 610100 in plasma over a uniform dose interval tau after administration of the last dose)
Time Frame: up to 42 days
multiple rising dose part
up to 42 days
Cmin,ss (minimum concentration of BIRT 2584 XX and BI 610100 in plasma at steady state over a uniform dosing interval tau)
Time Frame: up to 42 days
multiple rising dose part
up to 42 days
AUCtau,ss (area under the concentration-time curve of BIRT 2584 XX and BI 610100 in plasma at steady state over a uniform dosing interval tau)
Time Frame: up to 42 days
multiple rising dose part
up to 42 days
λz,ss (terminal rate constant of BIRT 2584 XX and BI 610100 in plasma at steady state)
Time Frame: up to 42 days
multiple rising dose part
up to 42 days
t1/2,ss (terminal half-life of BIRT 2584 XX and BI 610100 in plasma at steady state)
Time Frame: up to 42 days
multiple rising dose part
up to 42 days
MRTpo,ss (mean residence time of BIRT 2584 XX and BI 610100 in the body at steady state after po administration)
Time Frame: up to 42 days
multiple rising dose part
up to 42 days
CL/F,ss (apparent clearance of BIRT 2584 XX from plasma at steady state after extravascular multiple dose administration)
Time Frame: up to 42 days
multiple rising dose part
up to 42 days
Vz/F,ss (apparent volume of distribution of BIRT XX 2584 during the terminal phase λz at steady state following extravascular administration)
Time Frame: up to 42 days
multiple rising dose part
up to 42 days
Aet1-t2,ss (amount of BIRT 2584 XX and BI 610100 that is eliminated in urine at steady state from the time point t1 to time point t2)
Time Frame: up to 30 days
multiple rising dose part
up to 30 days
fet1-t2,ss (fraction of BIRT 2584 XX and BI 610100 eliminated in urine at steady state from time point t1 to the time point t2)
Time Frame: up to 30 days
multiple rising dose part
up to 30 days
Accumulation ratio of the analyte in plasma at steady state at the end of dosing expressed as a ratio of Cmax after the last dose to Cmax after the first dose (RA,Cmax)
Time Frame: up to 42 days
multiple rising dose part
up to 42 days
Accumulation ratio of the analyte in plasma at steady state at the end of dosing expressed as a ratio of AUCtau after the last dose to AUCtau after the first dose (RA,AUC)
Time Frame: up to 42 days
multiple rising dose part
up to 42 days
Assessment of receptor occupancy
Time Frame: up to 42 days
determined by a competitive binding assay using anti-Lymphocyte function associated antigen-1 (LFA-1) antibody fragment as competitor
up to 42 days
Assessment of ex vivo suppression of superantigen (SEB)-induced Interleukin (IL)-2 production
Time Frame: up to 42 days
up to 42 days
Total number of white blood cells and leukocyte differential cell count
Time Frame: up to 42 days
up to 42 days

Collaborators and Investigators

This is where you will find people and organizations involved with this study.

Sponsor

Sponsor

The organization or person who initiates the study and who has authority and control over the study.
Boehringer Ingelheim

Publications and helpful links

The person responsible for entering information about the study voluntarily provides these publications. These may be about anything related to the study.

Helpful Links

Study record dates

These dates track the progress of study record and summary results submissions to ClinicalTrials.gov. Study records and reported results are reviewed by the National Library of Medicine (NLM) to make sure they meet specific quality control standards before being posted on the public website.

Study Major Dates

Study Start

Study Start

The actual date on which the first participant was enrolled in a clinical study. The "anticipated" study start date is the date that the researchers think will be the study start date.
January 1, 2005

Primary Completion (Actual)

Primary Completion

The date on which the last participant in a clinical study was examined or received an intervention to collect final data for the primary outcome measure. Whether the clinical study ended according to the protocol or was terminated does not affect this date. For clinical studies with more than one primary outcome measure with different completion dates, this term refers to the date on which data collection is completed for all the primary outcome measures. The "anticipated" primary completion date is the date that the researchers think will be the primary completion date for the study.
July 1, 2005

Study Registration Dates

First Submitted

First Submitted

The date on which the study sponsor or investigator first submitted a study record to ClinicalTrials.gov. There is typically a delay of a few days between the first submitted date and the record's availability on ClinicalTrials.gov (the first posted date).
October 2, 2014

First Submitted That Met QC Criteria

First Submitted That Met QC Criteria

The date on which the study sponsor or investigator first submits a study record that is consistent with National Library of Medicine (NLM) quality control (QC) review criteria. The sponsor or investigator may need to revise and submit a study record one or more times before NLM's QC review criteria are met. It is the responsibility of the sponsor or investigator to ensure that the study record is consistent with the NLM QC review criteria.
October 2, 2014

First Posted (Estimate)

First Posted

The date on which the study record was first available on ClinicalTrials.gov after National Library of Medicine (NLM) quality control (QC) review has concluded. There is typically a delay of a few days between the date the study sponsor or investigator submitted the study record and the first posted date.
October 6, 2014

Study Record Updates

Last Update Posted (Estimate)

Last Update Posted

The most recent date on which changes to a study record were made available on ClinicalTrials.gov. There may be a delay between when the changes were submitted to ClinicalTrials.gov by the study's sponsor or investigator (the last update submitted date) and the last update posted date.
October 6, 2014

Last Update Submitted That Met QC Criteria

Last Update Submitted That Met QC Criteria

The most recent date on which the study sponsor or investigator submitted changes to a study record that are consistent with National Library of Medicine (NLM) quality control (QC) review criteria. It is the responsibility of the sponsor or investigator to ensure that the study record is consistent with the NLM QC review criteria.
October 2, 2014

Last Verified

Last Verified

The most recent date on which the study sponsor or investigator confirmed the information about a clinical study on ClinicalTrials.gov as accurate and current. If a study with a recruitment status of recruiting; not yet recruiting; or active, not recruiting has not been confirmed within the past 2 years, the study's recruitment status is shown as unknown.
October 1, 2014

More Information

Terms related to this study

Other Study ID Numbers

Other Study ID Numbers

Identifiers or ID numbers other than the NCT number that are assigned to a clinical study by the study's sponsor, funders, or others. These numbers may include unique identifiers from other trial registries and National Institutes of Health grant numbers.
  • 1206.2

This information was retrieved directly from the website clinicaltrials.gov without any changes. If you have any requests to change, remove or update your study details, please contact register@clinicaltrials.gov. As soon as a change is implemented on clinicaltrials.gov, this will be updated automatically on our website as well.

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