Relative Bioavailability of Single Doses of Dabigatran Etexilate in Healthy Volunteers

NCT02173717 | Completed Phase 1

• 1 other identifier: 1160.100
• Study Type: interventional
• Target: 24
• Locations: 0 countries
• Sites: N/A

Brief Summary

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

Conditions

Healthy

Outcome Measures

Primary Outcomes (2)

• Area under the concentration-time curve over the time interval from 0 extrapolated to infinity (AUC0-inf) of total dabigatran

  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

  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 (30)

• AUC0-inf of free dabigatran

  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

  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

  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

  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

  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

Study Arms (1)

Dabigatran etexilate

EXPERIMENTAL

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

Dabigatran etexilate DRUG

150 mg Dabigatran etexilate

Also known as: Pradaxa®, BIBR 1048 MS

Dabigatran etexilate

Rifampicin DRUG

600 mg Rifampicin

Also known as: Rifa® 600

Dabigatran etexilate

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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)

Sponsors & Collaborators

• Boehringer Ingelheim: lead

MeSH Terms

Interventions

Dabigatran; Rifampin

Intervention Hierarchy (Ancestors)

Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Benzimidazoles; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Rifamycins; Heterocyclic Compounds, 4 or More Rings; Lactams, Macrocyclic; Macrocyclic Compounds; Polycyclic Compounds

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: June 20, 2014
• First Posted: June 25, 2014
• Study Start: June 1, 2009
• Primary Completion: July 1, 2009
• Last Updated: June 25, 2014

Record last verified: 2014-06