Relative Bioavailability of Oral Suspension of Rivaroxaban Compared to Standard Tablet

Phase 1

Completed

• Conditions: Biological Availability
• Interventions: Drug: Rivaroxaban (Xarelto, BAY59-7939)

• Registration Number: NCT01853800
• Lead Sponsor: Bayer

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.

Detailed Description

Not available

Study Timeline

• Study Start: 2013-05
• Study First Submitted: 2013-05-13
• Study First Submitted QC: 2013-05-13
• Study First Posted: 2013-05-15
• Primary Completion: 2013-07
• Study Completion: 2013-08
• Status Verified: 2017-01
• Last Update Submitted: 2017-01-20
• Last Update Posted: 2017-01-23

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 14

Inclusion Criteria

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

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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)

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Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
Rivaroxaban (Treatment B) suspension (BN03501), fed	Rivaroxaban (Xarelto, BAY59-7939)	Subjects received single oral dose of Rivaroxaban suspension 20 mg (Treatment B, Batch number BN03501) under fed conditions in any intervention period.
Rivaroxaban (Treatment D) IR tablet, fasted	Rivaroxaban (Xarelto, BAY59-7939)	Subjects received single oral dose of Rivaroxaban IR tablet 10 mg (Treatment D) under fasting conditions in any intervention period.
Rivaroxaban (Treatment A) suspension (BN03501), fasted	Rivaroxaban (Xarelto, BAY59-7939)	Subjects received single oral dose of Rivaroxaban suspension 10 mg (Treatment A, Batch number BN03501) under fasting conditions in any intervention period.
Rivaroxaban (Treatment C) suspension (BR05701), fasted	Rivaroxaban (Xarelto, BAY59-7939)	Subjects received single oral dose of Rivaroxaban suspension 10 mg (Treatment C, Batch number BR05701) under fasting conditions in any intervention period.

Primary Outcome Measures

Name	Time	Method
Area Under the Concentration Versus Time Curve From Zero to Infinity After a Single Dose (AUC)	0-72 hours
Area Under the Concentration Versus Time Curve From Zero to Infinity Divided by Dose (AUC/D)	0-72 hours
Maximum Observed Drug Concentration in Measured Matrix Divided by Dose (Cmax/D)	0-72 hours
Maximum Observed Drug Concentration in Measured Matrix After a Single Dose (Cmax)	0-72 hours

Secondary Outcome Measures

Name	Time	Method
Area Under the Concentration Versus Time Curve From Zero to Infinity Divided by Dose per Kilogram Body Weight (AUC,norm)	0-72 hours
Mean Residence Time (MRT)	0-72 hours
Maximum Observed Drug Concentration Divided by Drug Concentration at 24 hours (Cmax/C24h)	0-72 hours
Terminal Half Life (t1/2)	0-72 hours
Area Under the Concentration Versus Time Curve From Zero to Last Quantifiable Concentration [AUC(0tlast)]	0-72 hours
Time to Reach Maximum Observed Drug Concentration (tmax)	0-72 hours
Maximum Observed Drug Concentration Divided by Dose per Kilogram Body Weight (Cmax,norm)	0-72 hours