Clinical trial NCT01853800: Relative Bioavailability of Oral Suspension of Rivaroxaban Compared to Standard Tablet
Official title: Single-dose, Open-label, Randomized, 4-way Crossover Study to Compare 10 mg of an Oral Suspension of Rivaroxaban Under Fasting (2 Different Batches) and 20 mg of an Oral Suspension of Rivaroxaban Under Fed Conditions to 10 mg of an Immediate Release Tablet Under Fasting Conditions in Healthy Subjects
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Biological Availability
Keywords: Relative bioavailability
Rivaroxaban
Lead sponsor: Bayer
Sponsor class: INDUSTRY
Collaborators: name: Janssen Research & Development, LLC
First posted: 2013-05-15
Enrollment: 14
Sex: MALE
Minimum age (years): 18
Maximum age (years): 55
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: CROSSOVER
Primary purpose: OTHER

Brief summary: Rivaroxaban is a substance developed for use in the treatment of blood coagulation disorders. Thrombosis (blood clots) can occur as a result of excessive coagulation activity in the blood vessels. Excessive coagulation activity can occur in children as well, and rivaroxaban is therefore being developed for the treatment of thromboembolic events in children and adolescents. As small children are often unable to swallow tablets, an oral suspension (mixture of a liquid containing finely distributed solids) has been developed which allows dosing according to body weight. The objective of this trial is to compare the bioavailability (proportion of a substance that remains available unchanged in the blood circulation) of a rivaroxaban oral solution with that of the rivaroxaban tablet approved for treatment. In order to evaluate the potential influence of food, the oral suspension containing 20 mg rivaroxaban will be taken after consuming food. In addition, the pharmacokinetics (concentrations of the drug and breakdown products (metabolites) in blood), safety and tolerability will be assessed.


Eligibility criteria: Inclusion Criteria:

* Healthy male subjects
* Age: 18 to 55 years (inclusive) at the first screening examination

Exclusion Criteria:

* Incompletely cured pre-existing diseases for which it can be assumed that the absorption, distribution, metabolism, elimination and effects of the study drugs will not be normal
* Known coagulation disorders (eg von Willebrand's disease, hemophilia)
* Known disorders with increased bleeding risk (eg periodontosis, hemorrhoids, acute gastritis, peptic ulcer)
* Known sensitivity to common causes of bleeding (eg nasal)
* Regular use of medicines
* Clinically relevant findings in the ECG (electrocardiogram) such as a second- or third-degree AV block, prolongation of the QRS complex over 120 msec or of the QTc-interval over 450 msec
* Clinically relevant findings in the physical examination
* Clinically relevant deviations of the screened laboratory parameters from reference ranges
* Participation in another clinical study during the preceding 3 months (Last Treatment from previous study to First Treatment of new study)

Primary outcomes:
measure: Area Under the Concentration Versus Time Curve From Zero to Infinity After a Single Dose (AUC)
timeFrame: 0-72 hours
measure: Area Under the Concentration Versus Time Curve From Zero to Infinity Divided by Dose (AUC/D)
timeFrame: 0-72 hours
measure: Maximum Observed Drug Concentration in Measured Matrix After a Single Dose (Cmax)
timeFrame: 0-72 hours
measure: Maximum Observed Drug Concentration in Measured Matrix Divided by Dose (Cmax/D)
timeFrame: 0-72 hours
Secondary outcomes:
measure: Area Under the Concentration Versus Time Curve From Zero to Infinity Divided by Dose per Kilogram Body Weight (AUC,norm)
timeFrame: 0-72 hours
measure: Area Under the Concentration Versus Time Curve From Zero to Last Quantifiable Concentration [AUC(0tlast)]
timeFrame: 0-72 hours
measure: Maximum Observed Drug Concentration Divided by Dose per Kilogram Body Weight (Cmax,norm)
timeFrame: 0-72 hours
measure: Mean Residence Time (MRT)
timeFrame: 0-72 hours
measure: Maximum Observed Drug Concentration Divided by Drug Concentration at 24 hours (Cmax/C24h)
timeFrame: 0-72 hours
measure: Time to Reach Maximum Observed Drug Concentration (tmax)
timeFrame: 0-72 hours
measure: Terminal Half Life (t1/2)
timeFrame: 0-72 hours
Other outcomes:
Locations:
city: Wuppertal
country: Germany
state: Nordrhein-Westfalen
Study officials:
affiliation: Bayer
name: Bayer Study Director
role: STUDY_DIRECTOR
References: