Safety, Tolerability and Pharmacokinetics of Oral BIBP 5371 CL in Healthy Male and Female Volunteers

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: BIBP 5371 CL tablet low dose; Drug: BIBP 5371 CL tablet high dose; Drug: Placebo drinking solution; Drug: BIBP 5371 CL solution; Other: High fat, high caloric breakfast; Drug: BIBP 5371 CL tablet; Drug: Placebo tablet

• Registration Number: NCT02256709
• Lead Sponsor: Boehringer Ingelheim

Brief Summary

Safety, tolerability and pharmacokinetics (including comparisons of different formulations and investigation of food effect)

Detailed Description

Not available

Study Timeline

• Study Start: 2004-04
• Primary Completion: 2004-08
• Status Verified: 2014-10
• Study First Submitted: 2014-10-02
• Study First Submitted QC: 2014-10-02
• Last Update Submitted: 2014-10-02
• Study First Posted: 2014-10-06
• Last Update Posted: 2014-10-06

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 70

Inclusion Criteria

• Healthy male and female volunteers
• Age 21 - 50 years
• Body mass index (BMI) 18.5 - 29.9 kg/m2

Read More

Exclusion Criteria

• Any finding of the medical examination (including blood pressure, pulse rate, respiratory rate, body temperature and ECG) deviating from normal
• Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
• Diseases of the central nervous system or psychiatric disorders or neurological disorders
• History of relevant orthostatic hypotension, fainting spells or blackouts
• Chronic or relevant acute infections
• History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator
• Intake of drugs with a long half-life (> 24 hours) within at least 1 month or less than 10 half-lives of the respective drug before enrolment in the study
• Use of any drugs which might influence the results of the trial (within 1 week prior to administration or during the trial)
• Participation in another trial with an investigational drug (within 2 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 (> 60 grams/day)
• Drug abuse
• Blood donation (≥ 100 mL within 4 weeks prior to administration or during the trial)
• Excessive physical activities (within the last week before the study)
• Any laboratory value outside the reference range of clinical relevance

In addition, for female subjects:

• Pregnancy
• Positive pregnancy test
• No adequate contraception e.g. oral contraceptives, intrauterine device, sterilisation

Females, who are not surgically sterile will be asked to additionally use barrier contraception methods (e.g. condoms) prior to administration of study medication, during the study and at least 1 month after release from the study

• Inability to maintain this adequate contraception during the whole study period
• Lactation period

Read More

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
BIBP 5371 CL tablet low dose	BIBP 5371 CL tablet low dose	to be compared with same daily dose level from single rising dose arm
BIBP 5371 CL tablet high dose	BIBP 5371 CL tablet high dose	to be compared with same daily dose level from single rising dose arm
Placebo drinking solution	Placebo drinking solution	-
BIBP 5371 CL drinking solution	BIBP 5371 CL solution	-
BIBP 5371 CL tablet high dose with food	High fat, high caloric breakfast	-
BIBP 5371 CL tablet high dose with food	BIBP 5371 CL tablet high dose	-
single rising dose BIBP 5371 CL	BIBP 5371 CL tablet	-
BIBP 5371 CL tablet low dose with food	High fat, high caloric breakfast	-
Placebo tablet	Placebo tablet	-
BIBP 5371 CL tablet low dose with food	BIBP 5371 CL tablet low dose	-

Primary Outcome Measures

Name	Time	Method
Number of patients with changes in electrocardiogram (ECG)	baseline, up to 8 days after drug administration
Number of patients with adverse events	baseline, up to 8 days after drug administration
Global tolerability assessment by the investigator on a verbal rating scale	up to 8 days after drug administration
Number of patients with changes in safety laboratory parameters	baseline, up to 8 days after drug administration
Number of patients with changes in vital signs	baseline, up to 8 days after drug administration	blood pressure, pulse rate, respiratory rate, body temperature

Secondary Outcome Measures

Name	Time	Method
λz (terminal rate constant in plasma)	up to 32 hours after drug administration
Aet1-t2 (amount of analyte eliminated in urine from the time point t1 to time point t2)	up to 32 hours after drug administration
t1/2 (terminal half-life of the analyte in plasma)	up to 32 hours after drug administration
MRTpo (mean residence time of the analyte in the body after po administration)	up to 32 hours after drug administration
CL/F (apparent clearance of the analyte in the plasma after extravascular administration)	up to 32 hours after drug administration
tmax (time from dosing to maximum concentration)	up to 32 hours after drug administration
%AUC0-tz (the percentage of the AUC0-∞ that is obtained by extrapolation)	up to 32 hours after drug administration
fet1-t2 (fraction of analyte eliminated in urine from time point t1 to time point t2)	up to 32 hours after drug administration
Cmax (maximum concentration of the analyte in plasma)	up to 32 hours after drug administration
AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)	up to 32 hours after drug administration
Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose)	up to 32 hours after drug administration
CLR,t1-t2 (renal clearance of the analyte from the time point t1 until the time point t2)	up to 32 hours after drug administration