The Effect of Multiple Doses of BI 187004 on the Single-dose Pharmacokinetics of Repaglinide and Bupropion in Healthy Male Volunteers

The Effect of Multiple Doses of BI 187004 on the Single-dose Pharmacokinetics of Repaglinide and Bupropion Following Oral Administration in Healthy Male Subjects (an Open-label, One-sequence Trial)

To assess the influence of BI 187004 on pharmacokinetics of CYP2C8 and CYP2B6 probe drugs repaglinide and bupropion as a means of predicting drug-drug interactions.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: repaglinide; Drug: BI 187004 tablet; Drug: bupropion extended release tablet

• Study Type: Interventional
• Enrollment (Actual): 18
• Phase: Phase 1

Contacts and Locations

Study Locations

• Germany
  • Biberach, Germany
    • 1307.20.1 Boehringer Ingelheim Investigational Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion criteria:

1. Healthy male subjects according to the investigator's assessment, based on a complete medical history including a physical examination, vital signs (BP, PR), 12-lead ECG, and clinical laboratory tests
2. Age of 18 to 55 years (incl.)
3. Body mass index (BMI) of 18.5 to 29.9 kg/m2 (incl.)
4. Signed and dated written informed consent prior to admission to the study in accordance with GCP and local legislation

Exclusion criteria:

1. Any finding in the medical examination (including BP, PR or ECG) is deviating from normal and judged as clinically relevant by the investigator
2. Repeated measurement of systolic blood pressure outside the range of 90 to 140 mmHg, diastolic blood pressure outside the range of 50 to 90 mmHg, or pulse rate outside the range of 50 to 90 bpm
3. Any laboratory value outside the reference range that the investigator considers to be of clinical relevance
4. Any evidence of a concomitant disease judged as clinically relevant by the investigator
5. Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
6. Cholecystectomy and/or surgery of the gastrointestinal tract that could interfere with the pharmacokinetics of the trial medication (except appendectomy and simple hernia repair)
7. Diseases of the central nervous system (including but not limited to any kind of seizures or stroke), and other relevant neurological or psychiatric disorders

Further exclusion criteria may apply.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Repaglinide + Bupropion + BI 187004; repaglinide tablets and bupropion tablets with and without concomitant administration of BI 187004	Drug: repaglinide; single dose on day 1 of visits 2 and 3; Drug: BI 187004 tablet; multiple doses on days 8-13 of visit 2 and days 1-7 of visit 3; Drug: bupropion extended release tablet; single dose on day 3 of visits 2 and 3

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Area under the concentration-time curve of repaglinide in plasma over the time interval from 0 to the last quantifiable data point	up to 48 h post dose
Maximum measured concentration of repaglinide in plasma	up to 48 h post dose
Area under the concentration-time curve of total bupropion in plasma over the time interval from 0 to the last quantifiable data point	up to 119 h post dose
Area under the concentration-time curve of S-bupropion in plasma over the time interval from 0 to the last quantifiable data point	up to 119 h post dose
Maximum measured concentration of total bupropion in plasma	up to 119 h post dose
Maximum measured concentration of S-bupropion in plasma	up to 119 h post dose

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim

Study record dates

Study Major Dates

• Study Start: December 1, 2014
• Primary Completion (Actual): March 1, 2015
• Study Completion (Actual): March 1, 2015

Study Registration Dates

• First Submitted: December 1, 2014
• First Submitted That Met QC Criteria: December 1, 2014
• First Posted (Estimate): December 3, 2014

Study Record Updates

• Last Update Posted (Estimate): May 12, 2015
• Last Update Submitted That Met QC Criteria: May 10, 2015
• Last Verified: May 1, 2015

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Hypoglycemic Agents; Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Psychotropic Drugs; Neurotransmitter Uptake Inhibitors; Membrane Transport Modulators; Antidepressive Agents; Dopamine Agents; Cytochrome P-450 Enzyme Inhibitors; Antidepressive Agents, Second-Generation; Cytochrome P-450 CYP2D6 Inhibitors; Dopamine Uptake Inhibitors; Bupropion; Repaglinide
• Other Study ID Numbers: 1307.20; 2013-005030-38 (EudraCT Number: EudraCT)