Relative Bioavailability of Oral Suspension of Rivaroxaban Compared to Standard Tablet

Bayer

Status and phase: Completed; Phase 1

Conditions: Biological Availability

Treatments: Drug: Rivaroxaban (Xarelto, BAY59-7939)

Study type: Interventional

Funder types: Industry

Identifiers

NCT01853800

16886

2013-001720-19 (EudraCT Number)

Details and patient eligibility

About

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.

Enrollment: 14 patients

Sex: Male

Ages: 18 to 55 years old

Volunteers: Accepts Healthy Volunteers

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)

Trial design

Primary purpose: Other

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

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14 participants in 4 patient groups

Rivaroxaban (Treatment A) suspension (BN03501), fasted

Experimental group

Description:

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

Treatment:

Drug: Rivaroxaban (Xarelto, BAY59-7939)

Rivaroxaban (Treatment B) suspension (BN03501), fed

Experimental group

Description:

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

Treatment:

Drug: Rivaroxaban (Xarelto, BAY59-7939)

Rivaroxaban (Treatment C) suspension (BR05701), fasted

Experimental group

Description:

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

Treatment:

Drug: Rivaroxaban (Xarelto, BAY59-7939)

Rivaroxaban (Treatment D) IR tablet, fasted

Experimental group

Description:

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

Treatment:

Drug: Rivaroxaban (Xarelto, BAY59-7939)