Relative Bioavailability of Oral Suspension of Rivaroxaban Compared to Standard Tablet

NCT01853800 | Completed Phase 1

• 2 other identifiers: 168862013-001720-19
• Study Type: interventional
• Target: 14
• Locations: 1 country
• Sites: 1

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.

Conditions

Biological Availability

Keywords

Relative bioavailability; Rivaroxaban

Outcome Measures

Primary Outcomes (4)

• 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 After a Single Dose (Cmax)

  0-72 hours

• Maximum Observed Drug Concentration in Measured Matrix Divided by Dose (Cmax/D)

  0-72 hours

Secondary Outcomes (7)

• Area Under the Concentration Versus Time Curve From Zero to Infinity Divided by Dose per Kilogram Body Weight (AUC,norm)

  0-72 hours

• Area Under the Concentration Versus Time Curve From Zero to Last Quantifiable Concentration [AUC(0tlast)]

  0-72 hours

• Maximum Observed Drug Concentration Divided by Dose per Kilogram Body Weight (Cmax,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

Study Arms (4)

Rivaroxaban (Treatment A) suspension (BN03501), fasted

EXPERIMENTAL

Subjects received single oral dose of Rivaroxaban suspension 10 mg (Treatment A, Batch number BN03501) under fasting conditions in any intervention period.

Drug: Rivaroxaban (Xarelto, BAY59-7939)

Rivaroxaban (Treatment B) suspension (BN03501), fed

EXPERIMENTAL

Subjects received single oral dose of Rivaroxaban suspension 20 mg (Treatment B, Batch number BN03501) under fed conditions in any intervention period.

Drug: Rivaroxaban (Xarelto, BAY59-7939)

Rivaroxaban (Treatment C) suspension (BR05701), fasted

EXPERIMENTAL

Subjects received single oral dose of Rivaroxaban suspension 10 mg (Treatment C, Batch number BR05701) under fasting conditions in any intervention period.

Drug: Rivaroxaban (Xarelto, BAY59-7939)

Rivaroxaban (Treatment D) IR tablet, fasted

EXPERIMENTAL

Subjects received single oral dose of Rivaroxaban IR tablet 10 mg (Treatment D) under fasting conditions in any intervention period.

Drug: Rivaroxaban (Xarelto, BAY59-7939)

Interventions

Rivaroxaban (Xarelto, BAY59-7939) DRUG

Rivaroxaban (Treatment A) suspension (BN03501), fasted; Rivaroxaban (Treatment B) suspension (BN03501), fed; Rivaroxaban (Treatment C) suspension (BR05701), fasted; Rivaroxaban (Treatment D) IR tablet, fasted

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

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

You may not qualify if:

• 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)

Sponsors & Collaborators

• Bayer: lead
• Janssen Research & Development, LLC: collaborator

Study Sites (1)

Unknown Facility

Wuppertal, North Rhine-Westphalia, 42096, Germany

Location

Related Links

• Click here to find information about studies related to Bayer Healthcare products conducted in Europe.

MeSH Terms

Interventions

Rivaroxaban

Intervention Hierarchy (Ancestors)

Thiophenes; Sulfur Compounds; Organic Chemicals; Morpholines; Oxazines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Study Officials

• Bayer Study Director

  Bayer

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: May 13, 2013
• First Posted: May 15, 2013
• Study Start: May 1, 2013
• Primary Completion: July 1, 2013
• Study Completion: August 1, 2013
• Last Updated: January 23, 2017

Record last verified: 2017-01

Locations

DE (1)