Bioavailability of BI 1356 Administered With and Without Food to Healthy Male and Female Subjects

Relative Bioavailability of a 5 mg BI 1356 Tablet Administered With and Without Food to Healthy Male and Female Subjects in an Open, Randomised, Single Dose, Two-way Crossover, Phase I Trial

To investigate the food effect on the relative bioavailability and pharmacokinetics of a 5 mg BI 1356 tablet administered as a single dose

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: BI 1356

• Study Type: Interventional
• Enrollment (Actual): 32
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 50 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Healthy males and females 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 ≥ 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 good clinical practice (GCP) and the local legislation

Exclusion Criteria:

• Any finding of the medical examination deviating from normal and of clinical relevance. Repeated measurement of a systolic blood pressure greater than 140 mm Hg or diastolic blood pressure greater than 90 mm Hg
• 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 within one month or less than 10 half-lives of the respective drug prior to first study drug administration and during the trial except if a relevant interaction can be ruled out
• Participation in another trial with an investigational drug within two months prior to first study drug 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 (average consumption of more than 20 g/day in females and 30 g/day in males)
• Drug abuse
• Blood donation (more than 100 mL within four weeks prior to the start of study)
• 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 torsades de points (e.g., heart failure, hypokalemia, family history of Long QT Syndrome)

For female subjects:

• Positive pregnancy test, pregnancy or planning to become pregnant during the study or within 2 months after study completion
• No adequate contraception during the study and until 2 months after study completion, i.e. not any of the following: implants, injectables, combined oral contraceptives, intrauterine device (IUD) , sexual abstinence for at least 1 month prior to enrolment, vasectomised partner (vasectomy performed at least 1 year prior to enrolment), or surgical sterilisation (including hysterectomy). Females, who do not have a vasectomised partner, are not sexually abstinent or surgically sterile will be asked to use an additional barrier method (e.g. condom, diaphragm with spermicide)
• Lactation

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Fed administration of BI 1356	Drug: BI 1356
Active Comparator: Fasted administration of BI 1356	Drug: BI 1356

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Area under the concentration-time curve of BI 1356 in plasma over the time interval from 0 to 72 h (AUC0-72)	up to 72 hours after start of treatment
Maximum measured concentration (Cmax) of BI 1356 in plasma	up to 96 hours after start of treatment

Secondary Outcome Measures

Outcome Measure	Time Frame
Number of patients with adverse events	up to 11 weeks
Assessment of tolerability on a 4-point scale by investigator	14 days after last study drug administration
Area under the concentration-time curve of BI 1356 in plasma at different time points	up to 96 hours after start of treatment
Time from dosing to the maximum concentration (tmax) of BI 1356 in plasma	up to 96 hours after start of treatment
Terminal elimination rate constant (λz) in plasma	up to 96 hours after start of treatment
Terminal half-life (t1/2) of BI 1356 in plasma	up to 96 hours after start of treatment
Mean residence time of BI 1356 in the body after oral administration (MRTpo)	up to 96 hours after start of treatment
Apparent clearance of BI 1356 in the plasma after extravascular administration (CL/F)	up to 96 hours after start of treatment
Apparent volume of distribution during the terminal phase λz following an extravascular dose (Vz/F)	up to 96 hours after start of treatment

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim

Publications and helpful links

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start: October 1, 2008
• Primary Completion (Actual): December 1, 2008

Study Registration Dates

• First Submitted: July 4, 2014
• First Submitted That Met QC Criteria: July 4, 2014
• First Posted (Estimate): July 8, 2014

Study Record Updates

• Last Update Posted (Estimate): July 8, 2014
• Last Update Submitted That Met QC Criteria: July 4, 2014
• Last Verified: July 1, 2014

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Hypoglycemic Agents; Physiological Effects of Drugs; Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Hormones; Hormones, Hormone Substitutes, and Hormone Antagonists; Protease Inhibitors; Incretins; Dipeptidyl-Peptidase IV Inhibitors; Linagliptin
• Other Study ID Numbers: 1218.34