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Multiple Doses of BI 207127 NA, BI 201335 NA Followed by the Combination of BI 207127 NA and BI 201335 NA in Healthy Male Volunteers

Information source: Boehringer Ingelheim
ClinicalTrials.gov processed this data on August 23, 2015
Link to the current ClinicalTrials.gov record.

Condition(s) targeted: Healthy

Intervention: BI 207127 NA (Drug); BI 201335 NA (Drug); Midazolam (Drug); Tolbutamide (Drug)

Phase: Phase 1

Status: Terminated

Sponsored by: Boehringer Ingelheim


Study to investigate the pharmacokinetic drug-drug interaction potential of BI 207127 NA and BI 201335 NA on each other at steady-state and to quantify the effect of BI 207127 NA, and BI 207127 NA combined with BI 201335 NA, on the activity of CYP 2C9 and CYP 3A4 using the probe substrates tolbutamide (CYP 2C9) and midazolam (CYP 3A4).

Clinical Details

Official title: An Open-label, Fixed Sequence Phase I Study in Healthy Male Volunteers to Assess Sequentially the Effects of Multiple Doses of BI 207127 NA, BI 201335 NA Followed by the Combination of BI 207127 NA and BI 201335 NA, on the Single Dose Pharmacokinetics of Midazolam and Tolbutamide and on the Systemic Exposure of BI 207127 NA and BI 201335 NA

Study design: Intervention Model: Single Group Assignment, Masking: Open Label, Primary Purpose: Treatment

Primary outcome:

Steady-state Cmax (Maximum measured concentration of the analyte in plasma)

Steady-state AUC (Area under concentration-time curve)

Secondary outcome:

Cmax for several time points

Tmax (Time from dosing to the maximum measured concentration of the analyte in plasma)

Cx for several time points

AUC for several time points

CL/F (Total apparent clearance of the analyte in plasma following extravascular administration) for several time points

V/F (Apparent volume of distribution during following an extravascular dose) for several time points

t1/2 (Terminal half-life of the analyte in plasma)


Ratio for Cmax,Met at several time points

Ratio for AUC at several time points


Ae (amount of analyte eliminated in urine for different time points)

CLR (renal clearance of the analyte for different time points)

fe (fraction of analyte eliminated in urine for different time points)

Number of patients with adverse events

Assessment of tolerability on a 4-pointe scale by investigator


Minimum age: 21 Years. Maximum age: 50 Years. Gender(s): Male.


Inclusion Criteria:

- Healthy males (caucasian)

- Age ranging ≥ 21 and ≤ 50 years

- Body mass index (BMI) ≥ 19 and ≤ 29. 9 kg/m2

- Willing to complete all study-related activities

- Volunteers give their written informed consent prior to admission to the study

Exclusion criteria:

- Any finding of the medical examination (including blood pressure, pulse rate and

electrocardiogram) deviating from normal and of clinical relevance

- Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic,

immunological or hormonal disorders, clinically relevant electrolyte disturbances

- Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or

neurological disorders

- History of photosensitivity or recurrent rash

- History of orthostatic hypotension, fainting spells or blackouts

- Chronic or clinically 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: 00 hours) within at least one month or

less than ten half-lives of the respective drug before enrolment in the study or during the study

- Use of any drugs which might influence the results of the trial up to 7 days prior to

enrolment in the trial or during the trial

- vulnerable subjects (that is persons kept in detention)

- exclusion of contraindications or hypersensitivity to midazolam and / or tolbutamide

- Participation in another trial with an investigational drug (within two months prior

to administration or during the trial)

- Smoker (> 10 cigarettes or > 3 cigars of > 3 pipes/day)

- Inability to refrain from smoking on trial days

- Alcohol abuse (> 60 g/day)

- Drug abuse

- Blood donation (> 100 mL within four weeks prior to administration or during the


- Any laboratory value outside the reference range if indicative of underlying disease

or poor health

- Excessive physical activities within the last week before the trial or during the


- Hypersensitivity to treatment medication and/or related drugs of these classes

- A marked baseline prolongation of QT/QTc interval (e. g., repeated demonstration of a

QTcF, or QTcB interval >450 ms)

- Homozygous carriers of the UGT1A1 (uridine diphosphate glucuronosyltransferase 1A1)

enzyme polymorphism *28 and *60

Locations and Contacts

Additional Information

Starting date: July 2009
Last updated: July 17, 2014

Page last updated: August 23, 2015

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