Working…
ClinicalTrials.gov
ClinicalTrials.gov Menu

Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Single Rising Oral Doses and Multiple Rising Oral Doses of BI 1356 BS in Healthy Male Volunteers

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details.
 
ClinicalTrials.gov Identifier: NCT02183311
Recruitment Status : Completed
First Posted : July 8, 2014
Last Update Posted : July 8, 2014
Sponsor:
Information provided by (Responsible Party):
Boehringer Ingelheim

Brief Summary:
Study to examine the safety, tolerability, pharmacokinetics, and pharmacodynamics of BI 1356 BS administered to healthy male volunteers at single rising oral doses (1 mg, 2.5 mg, 5 mg, and 10 mg) and at multiple rising oral doses (2.5 mg, 5 mg, and 10 mg once daily for 12 days)

Condition or disease Intervention/treatment Phase
Healthy Drug: BI 1356 BS - single rising dose Drug: BI 1356 BS - multiple rising dose Drug: Placebo Phase 1

Layout table for study information
Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 56 participants
Allocation: Randomized
Intervention Model: Single Group Assignment
Masking: Double
Primary Purpose: Treatment
Official Title: Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Single Rising Oral Doses (1 to 10 mg) and Multiple Rising Oral Doses (2.5 to 10 mg Once Daily for 12 Days) of BI 1356 BS in Healthy Male Volunteers (a Randomised, Double-blind, Placebo Controlled Within Dose Groups Clinical Trial)
Study Start Date : June 2006
Actual Primary Completion Date : October 2006

Resource links provided by the National Library of Medicine

Drug Information available for: Linagliptin

Arm Intervention/treatment
Experimental: BI 1356 BS - single rising dose Drug: BI 1356 BS - single rising dose
Experimental: BI 1356 BS - multiple rising dose Drug: BI 1356 BS - multiple rising dose
Active Comparator: Placebo Drug: Placebo



Primary Outcome Measures :
  1. Number of patients with abnormal findings in physical examination [ Time Frame: Screening, up to 28 days ]
  2. Number of patients with clinically significant changes in Vital signs (blood pressure [BP], pulse rate [PR]) [ Time Frame: Screening, up to 28 days ]
  3. Number of patients with abnormal findings in 12-lead electrocardiogram (ECG) [ Time Frame: Screening, up to 28 days ]
  4. Number of patients with abnormal changes in laboratory parameters [ Time Frame: Screening, up to 28 days ]
  5. Number of patients with adverse events [ Time Frame: up to 49 days ]

Secondary Outcome Measures :
  1. Cmax (maximum measured concentration of the analyte in plasma) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  2. tmax (time from dosing to maximum measured concentration) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  3. AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  4. %AUCtz-∞ (the percentage of the AUCtz-∞ that is obtained by extrapolation) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  5. AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the time of the last quantifiable analyte plasma concentration) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  6. AUCt1-t2 (area under the concentration-time curve of the analyte in plasma over the time interval from the time point t1 to the time point t2) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  7. λz (terminal rate constant in plasma) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  8. t1/2 (terminal half-life of the analyte in plasma) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  9. MRTpo (mean residence time of the analyte in the body) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  10. CL/F (apparent clearance of the analyte in plasma after extravascular administration) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  11. Vz/F (apparent volume of distribution during the terminal phase λz following extravascular administration) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  12. Aet1-t2 (amount of analyte that is eliminated in urine from the time point t1 to the time point t2) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  13. fet1-t2 (fraction of analyte eliminated in urine from the time point t1 to the time point t2) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  14. CLR,t1-t2 (renal clearance of the analyte from the time point t1 until the time point t2) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  15. CLR,0-24,1 (renal clearance of the analyte from 0 until 24 hours after administration of the first dose) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  16. Cmin,ss (minimum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  17. Cavg (average concentration of the analyte in plasma at steady state) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  18. Cpre (predose concentration of the analyte in plasma) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  19. RA,Cmax based on Cmax [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  20. RA,AUC based on AUCτ [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  21. Emin (minimum Dipeptidyl-Peptidase IV (DPP-IV) activity [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  22. tmin (time to reach minimum DPP-IV activity) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]
  23. E24 (DPP-IV activity 24 hours after administration of single dose administration and the first dose of multiple dose administration) [ Time Frame: up to 192 h (single dose), up to 456 h (multiple dose) ]


Information from the National Library of Medicine

Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the contacts provided below. For general information, Learn About Clinical Studies.


Layout table for eligibility information
Ages Eligible for Study:   20 Years to 35 Years   (Adult)
Sexes Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria:

  • Subjects will be healthy male volunteers who meet the criteria below: Persons without clinically remarkable findings or clinically evident complications based on their concurrent illness, past medical history, physical examination, vital signs (blood pressure (BP), pulse rate (PR), and body temperature), 12-lead Electrocardiogram (ECG), and laboratory test results
  • Persons who are 20 or older and 35 or younger
  • Persons with a BMI 17.6 kg/m2 or more and 29.9 kg/m2 or less
  • Persons who are willing to participate in this trial before study initiation and who give their written consent in accordance with GCP (Good Clinical Practice, MHW Ordinance No. 28 dated March 27, 1997)

Exclusion Criteria:

  • Persons who deviate from the norm and who show clinical findings (BP, PR, and ECG) on consultation
  • Persons with any clinically relevant complications
  • Persons with gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immune, or hormonal disorders
  • Persons with central nervous system disorders (e.g., epilepsy), mental disorders, or neurological disorders
  • Persons with a history of significant orthostatic hypotension, syncopal attacks, or blackouts
  • Persons with chronic infection or severe acute infection
  • Persons with a history of severe allergy/hypersensitivity including allergies to drugs and inactive ingredients
  • Persons who will have received a drug with a long half-life (more than 24 hours) within the month before treatment in this trial, within a period 10 times longer than the half-life of each drug, or during the study
  • Persons who will have received a drug that may theoretically affect the study results based on the information obtained at the time of preparation of the protocol within the 10 days before treatment or during the study
  • Persons who will have participated in another trial of an investigational drug within the 4 months before treatment or during the study
  • Smokers (who smoke more than 10 cigarettes or 3 cigars or 3 pipes per day)
  • Persons who cannot abstain from smoking throughout the study
  • Persons who undoubtedly abuse alcohol
  • Persons who abuse drugs
  • Persons who donate blood of 100 mL or more within the 4 weeks before treatment
  • Persons who perform rigorous exercise (within the week before treatment or during the study)
  • Persons with any laboratory test result outside the reference range and for whom the result is considered a clinically relevant change
  • Persons who cannot obey the dieting rules of the trial site
  • Persons with any ECG value outside the reference range and who are of clinical importance. Examples include, but are not limited to, QRS interval>120 ms

Layout table for additonal information
Responsible Party: Boehringer Ingelheim
ClinicalTrials.gov Identifier: NCT02183311     History of Changes
Other Study ID Numbers: 1218.11
First Posted: July 8, 2014    Key Record Dates
Last Update Posted: July 8, 2014
Last Verified: July 2014
Additional relevant MeSH terms:
Layout table for MeSH terms
Linagliptin
Hypoglycemic Agents
Physiological Effects of Drugs
Incretins
Hormones
Hormones, Hormone Substitutes, and Hormone Antagonists
Dipeptidyl-Peptidase IV Inhibitors
Protease Inhibitors
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action