Relative Bioavailability Study in Healthy Subjects Comparing 2 Dry Powder Oral Suspensions of Rivaroxaban Under Fasting and 20 mg of an Oral Suspension of Rivaroxaban Under Fed Conditions to 10 mg of an Immediate Release Tablet Under Fasting Conditions

NCT02367027 | Completed Phase 1

• 2 other identifiers: 177692014-004337-69
• Study Type: interventional
• Target: 18
• 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 new oral suspension of rivaroxaban with a previously used oral suspension and with a rivaroxaban tablet approved for treatment. In order to evaluate the potential influence of food, the new 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

Pharmacokinetics

Keywords

Biological Availability; Relative Bioavailability Trial

Outcome Measures

Primary Outcomes (4)

• Plasma concentration of rivaroxaban characterized by AUC

  AUC:area under the concentration vs. time curve from zero to infinity after single (first) dose

  Dosing day(15 min, 30 min ,45 min ,1 ,1.5, 2, 2.5 ,3 , 4, 6,8,12,15 hours), at 48 hr after administration), at 72 hr after administration)

• Plasma concentration of rivaroxaban characterized by AUC/D

  AUC/D: AUC divided by dose

  Dosing day(15 min, 30 min ,45 min ,1 ,1.5, 2, 2.5 ,3 , 4, 6,8,12,15 hours),at 48 hr after administration),at 72 hr after administration)

• Plasma concentration of rivaroxaban characterized by Cmax

  Cmax: maximum drug concentration in plasma after single dose administration

  Dosing day(15 min, 30 min ,45 min ,1 ,1.5, 2, 2.5 ,3 , 4, 6,8,12,15 hours),at 48 hr after administration),at 72 hr after administration)

• Plasma concentration of rivaroxaban characterized by Cmax/D

  Cmax/D: Cmax divided by dose

  Dosing day(15 min, 30 min ,45 min ,1 ,1.5, 2, 2.5 ,3 , 4, 6,8,12,15 hours),at 48 hr after administration),at 72 hr after administration)

Study Arms (4)

Arm 1 - BAY59-7939

EXPERIMENTAL

10 mg oral suspension (dry powder) in fasted conditions

Drug: Rivaroxaban (Xarelto, BAY59-7939)

Arn 2 - BAY59-7939

EXPERIMENTAL

20 mg oral suspension (dry powder) in fed conditions.

Drug: Rivaroxaban (Xarelto, BAY59-7939)

Arm 3 - BAY59-7939

EXPERIMENTAL

10 mg oral suspension in fasted conditions

Drug: Rivaroxaban (Xarelto, BAY59-7939)

Arm 4 - BAY59-7939

EXPERIMENTAL

10 mg tablet in fasted conditions.

Drug: Rivaroxaban (Xarelto, BAY59-7939)

Interventions

Rivaroxaban (Xarelto, BAY59-7939) DRUG

Single dose of 10 mg oral suspension (dry powder) in fasted conditions.

Arm 1 - BAY59-7939

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
• White
• Body Mass Index (BMI): ≥18.0 and ≤29.9 kg/m2 at the screening visit.

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 (e.g. von Willebrand's disease, hemophilia)
• Known disorders with increased bleeding risk (e.g. periodontosis, hemorrhoids, acute gastritis, peptic ulcer)
• Known sensitivity to common causes of bleeding (e.g. nasal)
• Regular use of medicines and use of medication that may have an impact on the study objectives
• Clinically relevant findings in the ECG 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

Mannheim, Baden-Wurttemberg, 68167, Germany

Location

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
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: February 13, 2015
• First Posted: February 20, 2015
• Study Start: February 1, 2015
• Primary Completion: April 1, 2015
• Study Completion: June 1, 2015
• Last Updated: June 10, 2015

Record last verified: 2015-06

Locations

DE (1)