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Safety, Tolerance, and Pharmacokinetics of Single Oral Doses of BI 201335 NA and Bioavailability in Healthy Male Subjects

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ClinicalTrials.gov Identifier: NCT02182323
Recruitment Status : Completed
First Posted : July 8, 2014
Last Update Posted : July 18, 2014
Sponsor:
Information provided by (Responsible Party):
Boehringer Ingelheim

Brief Summary:
The objective of this study was to investigate the safety, tolerability, and pharmacokinetics of BI 201335 NA following administration of single rising doses from 4 mg to 1200 mg. In addition, the food effect on the bioavailability of BI 201335 NA (480 mg) was investigated.

Condition or disease Intervention/treatment Phase
Healthy Drug: BI 201335 NA Drug: Placebo solution Phase 1

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Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 74 participants
Allocation: Randomized
Intervention Model: Parallel Assignment
Masking: Single (Participant)
Primary Purpose: Treatment
Official Title: Safety, Tolerance, and Pharmacokinetics of Single Oral Doses of 4 mg, 16 mg, 48 mg, 120 mg, 240 mg, 480 mg, 800 mg, and 1200 mg BI 201335 NA (PEG 400/TRIS/Meglumine/Water Solution) in Healthy Male Subjects, in a Randomised Single Blind, Placebo Controlled Rising Dose Study, Followed With an Open-label Intra-subject Two-stage Crossover Pilot Bioavailability Comparison of 480 mg BI 201335 NA in a PEG 400/TRIS/Meglumine/Water Solution Coadministered With Food
Study Start Date : September 2006
Actual Primary Completion Date : December 2006

Resource links provided by the National Library of Medicine


Arm Intervention/treatment
Experimental: BI 201335 in single rising doses Drug: BI 201335 NA
Placebo Comparator: Placebo Drug: Placebo solution
Experimental: BI 201335 NA fasted or fed

two randomized sequences:

  1. BI 201335 NA or placebo fasted
  2. BI 201335 NA or placebo after high-fat breakfast
Drug: BI 201335 NA
Drug: Placebo solution



Primary Outcome Measures :
  1. Number of patients with abnormal findings in physical examination [ Time Frame: up to 12 days ]
  2. Number of patients with clinically significant changes in vital signs (blood pressure, pulse rate) [ Time Frame: up to 12 days ]
  3. Number of patients with abnormal findings in 12-lead ECG (electrocardiogram) [ Time Frame: up to 12 days ]
  4. Number of patients with abnormal changes in laboratory tests (haematology, clinical chemistry and urinalysis) [ Time Frame: up to 12 days ]
  5. Number of patients with adverse events [ Time Frame: up to 12 days ]
  6. Assessment of tolerability by investigator on a 4-point scale [ Time Frame: within 7 days after last trial procedure ]

Secondary Outcome Measures :
  1. Cmax (maximum concentration of the analyte in plasma) [ Time Frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 hours post-dose ]
  2. tmax (time from dosing to maximum concentration) [ Time Frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 hours post-dose ]
  3. AUC0-infinity (area under the concentration time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity) [ Time Frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 hours post-dose ]
  4. AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the last quantifiable data point) [ Time Frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 hours post-dose ]
  5. λz (terminal elimination rate constant in plasma) [ Time Frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 hours post-dose ]
  6. t1/2 (terminal half-life of the analyte in plasma) [ Time Frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 hours post-dose ]
  7. MRTpo (Mean residence time of the analyte in the body after oral administration) [ Time Frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 hours post-dose ]
  8. CL/F (apparent clearance of the analyte in the plasma after oral administration) [ Time Frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 hours post-dose ]
  9. Vz/F (apparent volume of distribution during the terminal phase λz following an oral dose) [ Time Frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 30, 36, 48, 60, 72, 84, 96 hours post-dose ]
  10. Aet1-t2 (amount of analyte that is eliminated in urine from the time point t1 to time point t2) [ Time Frame: Pre-dose and 0-4, 4-12, 12-24, 24-48 hours post-dose in the single rising dose phase ]
  11. fet1-t2 (fraction of analyte eliminated in urine from time point t1 to time point t2) [ Time Frame: Pre-dose and 0-4, 4-12, 12-24, 24-48 hours post-dose in the single rising dose phase ]
  12. CLR,t1-t2 (renal clearance of the analyte from the time point t1 until the time point t2) [ Time Frame: Pre-dose and 0-4, 4-12, 12-24, 24-48 hours post-dose in the single rising dose phase ]


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Ages Eligible for Study:   18 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 ECG (electrocardiogram), clinical laboratory tests
  • Age ≥18 and Age ≤50 years
  • BMI ≥18.5 and BMI ≤29.9 kg/m2 (Body Mass Index)
  • Signed and dated written informed consent prior to admission to the study in accordance with GCP (Good Clinical Practice) 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
  • Prior history of jaundice
  • 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 hours) 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 two months prior to administration or during the trial
  • Smoker (> 10 cigarettes or > 3 cigars or > 3 pipes/day)
  • Inability to refrain from smoking alcohol and on trial days
  • Alcohol abuse (more than 60 g/day)
  • Drug abuse
  • Blood donation (more than 100 mL within four weeks prior to administration or during the trial)
  • Excessive physical activities (within one week prior to administration or during the trial)
  • Any laboratory value outside the reference range that is 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 TdP (torsade de pointes) (e.g., heart failure, hypokalemia, family history of Long QT Syndrome)

Additional Information:
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Responsible Party: Boehringer Ingelheim
ClinicalTrials.gov Identifier: NCT02182323     History of Changes
Other Study ID Numbers: 1220.3
First Posted: July 8, 2014    Key Record Dates
Last Update Posted: July 18, 2014
Last Verified: July 2014
Additional relevant MeSH terms:
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Pharmaceutical Solutions