Relative Bioavailability of BI 10773 and Linagliptin in Healthy Male Volunteers

Relative Bioavailability of Multiple Doses BI 10773 50 mg and Linagliptin 5 mg After Concomitant Administration Compared to Multiple Doses of BI 10773 50 mg and Linagliptin 5mg Administered Alone to Healthy Male Volunteers (an Open-label, Randomised, Crossover, Clinical Phase I Study)

Study to investigate the relative bioavailability of BI 10773 and of linagliptin after concomitant multiple oral administration of 50 mg BI 10773 tablets and 5 mg linagliptin in comparison to 50 mg BI 10773 and 5 mg linagliptin given alone.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Linagliptin; Drug: BI 10773

• Study Type: Interventional
• Enrollment (Actual): 16
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 50 years (ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Healthy male volunteers according to the following criteria:

  • Based upon a complete medical history and physical examination including vital signs (BP (blood pressure), PR (pulse rate)), 12-lead ECG (electrocardiogram) and clinical laboratory tests
• Age 18 to 50 years (inclusive)
• BMI 18.5 to 29.9 kg/m2 (inclusive)
• 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
• 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
• 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 on trial days
• Alcohol abuse (more than 30 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

Study Plan

How is the study designed?

Design Details

• Primary Purpose: TREATMENT
• Allocation: RANDOMIZED
• Interventional Model: CROSSOVER
• Masking: NONE

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
EXPERIMENTAL: Sequence ABC; Treatment A: BI 10773 once daily from day 1 to 5; Treatment B: BI10773 and linagliptin once daily from day 1 to 7; Treatment C: Linagliptin once daily from day 1 to 7	Drug: Linagliptin; Drug: BI 10773
EXPERIMENTAL: Sequence CAB; Treatment C: Linagliptin once daily from day 1 to 7; Treatment A: BI 10773 once daily from day 1 to 5; Treatment B: BI10773 and linagliptin once daily from day 1 to 7	Drug: Linagliptin; Drug: BI 10773

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
AUCτ,ss (area under the concentration-time curve of the analyte in plasma at steady state over a uniform dosing interval τ)	up to day 8
Cmax,ss (maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ)	up to day 8

Secondary Outcome Measures

Outcome Measure	Time Frame
tmax,ss (time from last dosing to the maximum measured concentration of each analyte in plasma at steady state)	up to day 8
Urine glucose excretion (UGE)	Pre-dose and 0-2, 2-4, 4-8, 8-12, 12-24 hours after the last dosing of each visit
Plasma DPP-4 (Dipeptidyl-peptidase 4) inhibition	2 hours and 24 hours after last administration of study drug
Changes from baseline in physical examination	Baseline and within 5 days after last study drug administration
Changes from baseline in vital signs (blood pressure, pulse rate)	Baseline, day 1 and within 5 days after last study drug administration
Changes from baseline in 12-lead ECG (electrocardiogram)	Baseline and within 5 days after last study drug administration
Changes from baseline clinical laboratory tests	Baseline, day 1 and within 5 days after last study drug administration
Incidence of adverse events	Up to 56 days
Assessment of tolerability by investigator on a 4-point scale	Within 5 days after last study drug administration

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim

Publications and helpful links

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start: July 1, 2009
• Primary Completion (ACTUAL): September 1, 2009

Study Registration Dates

• First Submitted: June 20, 2014
• First Submitted That Met QC Criteria: June 20, 2014
• First Posted (ESTIMATE): June 24, 2014

Study Record Updates

• Last Update Posted (ESTIMATE): June 24, 2014
• Last Update Submitted That Met QC Criteria: June 20, 2014
• Last Verified: June 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; Sodium-Glucose Transporter 2 Inhibitors; Dipeptidyl-Peptidase IV Inhibitors; Empagliflozin; Linagliptin
• Other Study ID Numbers: 1245.30