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

NCT02182323 | Completed Phase 1

• 1 other identifier: 1220.3
• Study Type: interventional
• Target: 74
• Locations: 0 countries
• Sites: N/A

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.

Conditions

Healthy

Outcome Measures

Primary Outcomes (6)

• Number of patients with abnormal findings in physical examination

  up to 12 days

• Number of patients with clinically significant changes in vital signs (blood pressure, pulse rate)

  up to 12 days

• Number of patients with abnormal findings in 12-lead ECG (electrocardiogram)

  up to 12 days

• Number of patients with abnormal changes in laboratory tests (haematology, clinical chemistry and urinalysis)

  up to 12 days

• Number of patients with adverse events

  up to 12 days

• Assessment of tolerability by investigator on a 4-point scale

  within 7 days after last trial procedure

Secondary Outcomes (12)

• Cmax (maximum concentration of the analyte in plasma)

  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

• tmax (time from dosing to maximum concentration)

  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

• AUC0-infinity (area under the concentration time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)

  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

• 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)

  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

• λz (terminal elimination rate constant in plasma)

  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

Study Arms (3)

BI 201335 in single rising doses

EXPERIMENTAL

Drug: BI 201335 NA

Placebo

PLACEBO COMPARATOR

Drug: Placebo solution

BI 201335 NA fasted or fed

EXPERIMENTAL

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

Interventions

BI 201335 NA DRUG

BI 201335 NA fasted or fed; BI 201335 in single rising doses

Placebo solution DRUG

BI 201335 NA fasted or fed; Placebo

Eligibility Criteria

• Age: 18 Years - 50 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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)

Sponsors & Collaborators

• Boehringer Ingelheim: lead

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: SINGLE
• Who Masked: PARTICIPANT
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 2, 2014
• First Posted: July 8, 2014
• Study Start: September 1, 2006
• Primary Completion: December 1, 2006
• Last Updated: July 18, 2014

Record last verified: 2014-07