Phase 1
N=28
Bioequivalence Study in Healthy Subjects, 2*5 mg Tablets Rivaroxaban Versus 1*10 mg Tablet Rivaroxaban
Therapeutic Equivalency
Bottom Line
View on ClinicalTrials.gov: NCT01436526 ↗Enrolled (actual)
28
Serious AEs
0.0%
Results posted
Dec 2011
Primary outcome: Primary: Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity After Single Dose (AUC) Incl. Bioequivalence (BE) Evaluation — 1374; 1268 µg*hr/L — p=0.0438
Study Design & Population
- Study type
- Interventional
- Phase
- Phase 1
- Interventions
- Rivaroxaban (Xarelto, BAY59-7939) (Drug)
- Age
- Adult · 18+ yrs
- Sex
- Male
- Sponsor
- Bayer
- Primary completion
- Sep 2009
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity After Single Dose (AUC) Incl. Bioequivalence (BE) Evaluation |
1374; 1268 | 0.0438 sig |
| PRIMARY Area Under the Plasma Concentration Versus Time Curve From Time Zero to Last Quantifiable Concentration [AUC (0-tn)] Incl. Bioequivalence (BE) Evaluation |
1354; 1252 | 0.0514 |
| PRIMARY Maximum Observed Drug Concentration in Plasma After Single Dose Administration (Cmax) Incl. Bioequivalence (BE) Evaluation |
179.8; 161.1 | 0.0685 |
| SECONDARY Area Under the Plasma Concentration Versus Time Curve Divided by Dose Per kg Body Weight (AUCnorm) |
10.79; 9.957 | — |
| SECONDARY Maximum Observed Drug Concentration in Plasma After Single Dose Administration Divided by Dose Per kg Body Weight (Cmax, Norm) |
1.412; 1.265 | — |
| SECONDARY Mean Residence Time (MRT) |
8.874; 9.284 | — |
| SECONDARY Time to Reach Maximum Drug Concentration in Plasma After Single Dose (Tmax) |
2.50; 2.50 | — |
| SECONDARY Half-life Associated With the Terminal Slope (t½) |
8.932; 8.721 | — |
Summary
The drug investigated in this study is Rivaroxaban, a novel, once-daily, oral anticoagulant for the prevention (prophylaxis) of deep vein thrombosis (DVT) which may lead to a pulmonary embolism (PE) in people undergoing knee or hip replacement surgery.
The purpose of this study is to establish bioequivalence of 2 immediate-release tablet treatments with Rivaroxaban: 2*5 mg tablets and 1*10 mg tablet will be given to healthy volunteers under fasting conditions; they will be administered as single oral doses in 2 periods. Both periods will be separated by a 7-day washout phase. Thus, the bioequivalence represents the primary study objective. As a secondary objective, this treatment will be assessed in terms of safety and tolerability.
Bioequivalence will be evaluated and verified on the basis of pharmacokinetic data. Blood samples of the volunteers will be taken at specific points in time; these samples will be analyzed using various statistical methods to establish pharmacokinetic characteristics required to compare the 2 treatments. The planned treatments with Rivaroxaban will be considered bioequivalent if specific criteria defined in the study protocol are met.
The study will be conducted in one center in Germany. 28 subjects meeting the inclusion criteria will participate. They will be treated according to a single-dose, randomized, 2-way cross-over, non-placebo-controlled design.
Eligibility Criteria
Inclusion Criteria
- Healthy male subjects
- 18 to 45 years of age
- Body mass index (BMI) between 18 and 30 kg/m2
Exclusion Criteria
- Conspicuous findings (medical history, screening)
- History of relevant diseases (internal organs, central nervous system or other organs)
- Medical disorder, condition or history of such that would impair the subject's ability to participate or complete this study in the opinion of the investigator or the sponsor
- Febrile illness within 1 week before the start of the study
- History of severe allergies, non-allergic drug reactions, or multiple drug allergies
- Hypersensitivity to the investigational drug, the control agent and/or to inactive constituents
- Known coagulation disorders, known disorders with increased bleeding risk, known sensitivity to common causes of bleeding
Data sourced from ClinicalTrials.gov (NCT01436526). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.