CompletedNCT02173717Updated Jun 25, 2014

Relative Bioavailability of Single Doses of Dabigatran Etexilate in Healthy Volunteers

A Phase 1 interventional study of Dabigatran etexilate and Rifampicin in Healthy, sponsored by Boehringer Ingelheim. Completed. Open to participants aged 18 Years to 45 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2014-06-25.

Sponsored by Boehringer Ingelheim · Phase 1, Interventional, and Treatment

Phase: Phase 1
Study type: Interventional
Enrollment: 24
Allocation: Not applicable
Ages: 18 Years to 45 Years
Sex: All

Study summary

Study to investigate whether and to what extent the suggested P-glycoprotein (P-gp) inducer rifampicin affects plasma exposure of dabigatran.

Conditions studied

Healthy

In context

Lead sponsor

Boehringer Ingelheim is the lead sponsor of 2,245 studies on the registry; 58 are open to participants now.

Of its 162 completed or terminated interventional studies of FDA-regulated products, 116 (72%) have results posted.

Counted across the registry records on this site, refreshed daily.

Who can participate

Ages eligible: 18 Years to 45 Years
Sexes eligible: All
Accepts healthy volunteers: Yes

Inclusion criteria

Healthy male or female subjects according to the following criteria: based upon a complete medical history, including the physical examination, vital signs (BP, pulse rate), 12-lead ECG, clinical laboratory tests
Age ≥18 and Age ≤45 years
Body Mass Index (BMI) ≥18.5 and ≤29.9 kg/m2
Signed and dated written informed consent prior to admission to the study in accordance with GCP and the local legislation

Exclusion criteria

Exclusion Criteria:

Any gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological, or hormonal disorders
Subjects who in the investigator's judgement were perceived as having an increased risk of bleeding, for example because of:
- Hemorrhagic disorders or bleeding diathesis
- Occult blood in faeces or haematocryal
- Trauma or surgery within the last month or as long as an excessive risk of bleeding persisted after these events, or planned surgery during trial participation
- History of arteriovenous malformation or aneurysm
- History of gastroduodenal ulcer disease, gastrointestinal haemorrhage, and haemorrhoids
- History of intracranial, intraocular, spinal, retroperitoneal, or atraumatic intraarticular bleeding
- Use of drugs that may have interfered with haemostasis during trial conduct (e.g. acetylic salicylic acid or other non-steroidal anti-inflammatory drugs)
- Relevant surgery of gastrointestinal tract
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 allergy/hypersensitivity (including drug allergy) which was deemed relevant to the trial as judged by the investigator
Use of drugs which might have reasonably influenced the results of the trial based on the knowledge at the time of protocol preparation within four weeks prior to administration or during the trial, especially inhibitors or inducers of P-gp, CYP3A4, CYP2C9, or CYP2C19 trial (comment: CYP3A4 inhibitors are for example azole antimycotics, macrolides or grapefruit juice, CYP3A inducers are for example St. John's Wort or certain anticonvulsants)
Intake of medication, which influences the blood clotting, i.e. acetylsalicylic acid, nonsteroidal anti-rheumatic drugs, cumarin, etc. within 14 days prior to screening or during the trial
Participation in another trial with an investigational drug within one month prior to administration or during the trial
Alcohol abuse (more than 60 g/day in males, more than 40 g/day in females)
Drug abuse
Blood donation (more than 100 mL within 4 weeks prior to administration)
Any laboratory value outside the reference range that was of clinical relevance
Inability to comply with dietary regimen of study centre
Previous intake of rifampicin
For female subjects:
- Pregnancy / positive pregnancy test, or planning to become pregnant during the study or within 1 month of study completion
- No adequate contraception in women of childbearing potential
- Lactation period

Study design

Phase: Phase 1
Primary purpose: Treatment
Allocation: Not applicable
Intervention model: Single group
Masking: None (open label)
Enrollment: 24 participants (actual)

Study arms

Experimental
Dabigatran etexilate
Four treatments of 150 mg Dabigatran etexilate (single oral administration) in a fixed sequence. 1. Single oral administration of dabigatran etexilate on Day 1; 2. Oral administration of 600 mg rifampicin q.d. in the evening for 7 days (Days 2 to 8) followed by an oral morning dose of dabigatran etexilate on Day 9; 3. Single oral administration of dabigatran etexilate on Day 16, after 7 days of rifampicin washout; 4. Single oral administration of dabigatran etexilate on Day 23, after 14 days of rifampicin washout
Drug: Dabigatran etexilate · Drug: Rifampicin

Interventions

DrugDabigatran etexilate
150 mg Dabigatran etexilate
Also known as: Pradaxa®, BIBR 1048 MS
DrugRifampicin
600 mg Rifampicin
Also known as: Rifa® 600

What researchers measure

Primary outcomes

Area under the concentration-time curve over the time interval from 0 extrapolated to infinity (AUC0-inf) of total dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Maximum measured concentration (Cmax) of total dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 334hours after treatment on Day1, 9, 16 and 23

Secondary outcomes

AUC0-inf of free dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Cmax of free dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Cmax of dabigatran etexilate
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Time from dosing to the maximum concentration (tmax) of dabigatran etexilate
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Cmax of BIBR 1087SE
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
tmax of BIBR 1087SE
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Cmax of BIBR 951BS
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
tmax of BIBR 951BS
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Area under the concentration-time curve over the time interval from 0 to the time of the last quantifiable data point (AUC0-tz) of free dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
AUC0-tz of total dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Area under the concentration-time curve over the time interval from timepoints t1 to t2 (AUCt1-t2) of free dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
AUCt1-t2 of total dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Area under the concentration-time curve over the time interval from 0 to 24 h (AUC0-24) of free dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
AUC0-24 of total dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
tmax of free dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
tmax of total dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Terminal rate constant (λz) of free dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
λz of total dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Terminal half-life (t1/2) of free dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
t1/2 of total dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Mean residence time after oral administration (MRTpo) of free dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
MRTpo of total dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Apparent clearance after extravascular administration (CL/F) of free dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
CL/F of total dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Apparent volume of distribution during the terminal phase λz following an extravascular dose (Vz/F) of free dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Vz/F of total dabigatran
Time frame: 30 min pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 34 hours after treatment on Day1, 9, 16 and 23
Amount that is eliminated in urine from the time interval 0- 24h (Ae0-24) of total dabigatran
Time frame: Day 1 and 9
Fraction excreted unchanged in urine from time point 0-24h (fe0-24) of total dabigatran
Time frame: Day 1 and 9
Renal clearance from the time point 0 until the point 0-24h (CLR, 0-24) of total dabigatran
Time frame: Day 1 and 9
Ratio of 6-ß-hydroxycortisol/cortisol in morning spot urine as a marker of CYP 3A induction
Time frame: Day 1 and 9

Study locations

No study locations are listed for this record.

Updates

Tracking since Sep 25, 2026

No changes since tracking began. The registry record was last updated on Jun 25, 2014, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗

Registry details

Key details

Study ID: NCT02173717
Lead sponsor: Boehringer Ingelheim
Responsible party: Sponsor
First posted: Jun 25, 2014
Start date: Jun 2009
Primary completion: Jul 2009
Last update: Jun 25, 2014

View the source record on ClinicalTrials.gov ↗

Not currently enrolling

This study is completed, as verified in Jun 2014. You cannot join it, but the record below documents what was studied.

Follow this study

Get an email when the registry record changes — status, dates, results — or when someone posts here.

Discussion

Questions and observations about this study, from anyone following it. Not medical advice, and not a channel to the study team — their contact details are on the registry record.

Sign in to join the discussion. Reading takes no account; posting does. You choose a display name, and a pseudonym is the default.

Nothing here yet. If you are running this trial, taking part in it, or weighing whether to, this is the place to say so.

Other studies from this sponsor

Boehringer Ingelheim

Start the discussion