Working…
ClinicalTrials.gov
ClinicalTrials.gov Menu

Safety, Tolerability and Pharmacokinetics of BI 653048 H3PO4 Oral Drinking Solution 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: NCT02217644
Recruitment Status : Completed
First Posted : August 15, 2014
Last Update Posted : August 15, 2014
Sponsor:
Information provided by (Responsible Party):
Boehringer Ingelheim

Brief Summary:
  • Investigation of safety and tolerability of BI 653048 H3PO4 following the administration of single rising doses of an aqueous solution in healthy male subjects
  • Pharmacokinetic and pharmacodynamic characteristics of BI 653048, including the investigation of dose proportionality
  • Investigation of relative bioavailability of capsules versus aqueous solution

Condition or disease Intervention/treatment Phase
Healthy Drug: BI 653048 H3PO4 solution Drug: BI 653048 H3PO4 low dose capsule Drug: BI 653048 H3PO4 high dose capsule Drug: Placebo Phase 1

Layout table for study information
Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 80 participants
Allocation: Randomized
Intervention Model: Parallel Assignment
Masking: Single
Primary Purpose: Treatment
Official Title: Safety, Tolerability and Pharmacokinetics of BI 653048 H3PO4 Oral Drinking Solution in Healthy Male Volunteers (Dose Range: 0.1 mg - 1500 mg). A Singleblind (Within Dose Groups), Randomised, Placebo-controlled Within Dose Groups, Single Rising Dose Phase I Study
Study Start Date : November 2008
Actual Primary Completion Date : June 2009

Arm Intervention/treatment
Experimental: BI 653048 H3PO4 solution
single rising doses
Drug: BI 653048 H3PO4 solution
Experimental: BI 653048 H3PO4 low dose capsule Drug: BI 653048 H3PO4 low dose capsule
Experimental: BI 653048 H3PO4 high dose capsule Drug: BI 653048 H3PO4 high dose capsule
Placebo Comparator: Placebo Drug: Placebo



Primary Outcome Measures :
  1. Number of patients with clinically significant findings in vital signs [ Time Frame: up to 10 days after drug administration ]
    blood pressure (BP), pulse rate (PR) respiratory rate (RR), oral body temperature (T), orthostatic test

  2. Number of patients with clinically significant findings in ECG [ Time Frame: up to 10 days after drug administration ]
  3. Number of patients with clinically significant findings in laboratory tests [ Time Frame: up to 10 days after drug administration ]
  4. Number of patients with adverse events [ Time Frame: up to 10 days after drug administration ]
  5. Assessment of tolerability performed by the investigator on a four-point scale [ Time Frame: up to 10 days after drug administration ]

Secondary Outcome Measures :
  1. Cmax (maximum measured concentration of the analyte in plasma) [ Time Frame: up to 72 hours after drug administration ]
  2. tmax (time from dosing to maximum measured concentration) [ Time Frame: up to 72 hours after drug administration ]
  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 72 hours after drug administration ]
  4. %AUCtz-∞ (the percentage of the AUC0-∞ that is obtained by extrapolation) [ Time Frame: up to 72 hours after drug administration ]
  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 data point) [ Time Frame: up to 72 hours after drug administration ]
  6. AUCt1-t2 (Area under the concentration-time curve of the analyte in plasma over the time interval t1 to t2) [ Time Frame: up to 72 hours after drug administration ]
  7. λz (terminal rate constant in plasma) [ Time Frame: up to 72 hours after drug administration ]
  8. t1/2 (terminal half-life of the analyte in plasma) [ Time Frame: up to 72 hours after drug administration ]
  9. MRTp.o. (mean residence time of the analyte in the body after oral administration) [ Time Frame: up to 72 hours after drug administration ]
  10. CL/F (total/apparent clearance of the analyte in plasma after extravascular administration) [ Time Frame: up to 72 hours after drug administration ]
  11. Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose) [ Time Frame: up to 72 hours after drug administration ]
  12. Aet1-t2 (amount of analyte eliminated in urine from the time point t1 to time point t2) [ Time Frame: up to 48 hours after drug administration ]
  13. fet1-t2 (fraction of analyte eliminated in urine from time point t1 to time point t2) [ Time Frame: up to 48 hours after drug administration ]
  14. CLR,t1-t2 (renal clearance of the analyte from the time point t1 until the time point t2) [ Time Frame: up to 48 hours after drug administration ]
  15. Dose-normalised Cmax [ Time Frame: up to 72 hours after drug administration ]
  16. Dose-normalized AUC0-∞ [ Time Frame: up to 72 hours after drug administration ]
  17. Emax (maximum measured concentration of the biomarker in blood or serum) [ Time Frame: up to 72 hours after drug administration ]
  18. Emin (minimum measured concentration of the biomarker in blood or serum) [ Time Frame: up to 72 hours after drug administration ]
  19. Tmin (time from dosing to minimum measured concentration of the biomarker) [ Time Frame: up to 72 hours after drug administration ]
  20. Tmax (time from dosing to maximum measured concentration of the biomarker) [ Time Frame: up to 72 hours after drug administration ]
  21. AUECt1-t2 (area under the concentration-time curve of the biomarker in the blood over the time interval from t1 to t2) [ Time Frame: up to 72 hours after drug administration ]
  22. AUECbelow_base (area under the baseline corrected concentration-time curve of the biomarker) [ Time Frame: up to 72 hours after drug administration ]
  23. AUECabove_base (area above the baseline corrected concentration-time curve of the biomarker) [ Time Frame: up to 72 hours after drug administration ]
  24. Expression of glucocorticoid responsive genes [ Time Frame: up to 72 hours after drug administration ]


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:   21 Years to 50 Years   (Adult)
Sexes Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria:

  • Healthy males according to the following criteria: Based upon a complete medical history, including the physical examination, vital signs (blood pressure (BP), pulse rate (PR)), 12-lead electrocardiogram (ECG), clinical laboratory tests
  • Age ≥21 years and ≤50 years
  • Body Mass Index (BMI) ≥18.5 kg/m2 and BMI ≤29.9 kg/m2
  • Signed and dated written informed consent prior to admission to the trial in accordance with Good Clinical Practice (GCP) and the local legislation

Exclusion Criteria:

  • Any finding of the medical examination (including BP, 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
  • Surgery of the gastrointestinal tract (except appendectomy)
  • 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 drug or its excipients)
  • Intake of drugs with a long half-life (>24 h) 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 or that prolong the QT/QTc interval 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 2 months prior to administration or during the trial
  • Smoker (>10 cigarettes or >3 cigars or >3 pipes/day)
  • Inability to refrain from smoking on trial days
  • Alcohol abuse (more than 60 g/day)
  • Drug abuse
  • Blood donation (more than 100 mL within 4 weeks prior to administration or during the trial)
  • Excessive physical activities (within 1 week prior to administration or during the trial)
  • Any laboratory value outside the reference range that was of clinical relevance
  • Inability to comply with dietary regimen of trial site
  • A marked baseline prolongation of QT/QTc interval (e.g., repeated demonstration of a QTc interval >450 ms)
  • A history of additional risk factors for Torsades des Pointes (e.g., heart failure, hypokalaemia, family history of Long QT Syndrome)
  • Not willing to use adequate contraception (condom use plus another form of contraception e.g., spermicide, oral contraceptive taken by female partner, sterilisation, intrauterine device) during the whole trial period from the time of the first intake of trial drug until 3 months after the last intake

Additional Information:
Publications automatically indexed to this study by ClinicalTrials.gov Identifier (NCT Number):
Layout table for additonal information
Responsible Party: Boehringer Ingelheim
ClinicalTrials.gov Identifier: NCT02217644     History of Changes
Other Study ID Numbers: 1262.1
First Posted: August 15, 2014    Key Record Dates
Last Update Posted: August 15, 2014
Last Verified: August 2014
Additional relevant MeSH terms:
Layout table for MeSH terms
Pharmaceutical Solutions