Clinical trial NCT04511611: Study to Compare the Effect of the Formulations (Orally Disintegrating Tablet and Film-coated Tablet) on Bioequivalence of Drug Rivaroxaban (Xarelto) at Dose of 10 mg in Japanese Healthy Male Adult Subjects
Official title: Randomized, Non-blinded, Two-way Crossover Study to Assess Bioequivalence Between a Rivaroxaban 10 mg Orally Disintegrating Tablet Administered With Water or Without Water and a Rivaroxaban 10 mg Film-coated Tablet in Japanese Healthy Male Adult Subjects
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Clinical Pharmacology
Lead sponsor: Bayer
Sponsor class: INDUSTRY
Collaborators: name: Janssen Research & Development, LLC
First posted: 2020-08-13
Enrollment: 80
Sex: MALE
Minimum age (years): 20
Maximum age (years): 40
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: CROSSOVER
Primary purpose: BASIC_SCIENCE

Brief summary: Researchers in this study wanted to compare the effect of the formulation (orally disintegrating tablet and film-coated tablet) on the bioequivalence of drug Rivaroxaban (brand name: Xarelto) at dose of 10 mg in Japanese healthy male subjects aged 20 to 40 years. Rivaroxaban is an approved drug to be used for the prevention of events/diseases caused by blood clots. Currently, there are two formulations of Rivaroxaban available on the market in Japan and they are film-coated tablets and fine granules. To further improve patients' convenience, a new formulation, orally disintegrating tablet (ODT, a drug dosage form designed to be dissolved on the tongue rather than swallowed whole) is under development. The goal of this study was to compare the effect of this new formulation with film-coated tablets when taken with or without water.

Participants in this study received one oral dose of rivaroxaban 10 mg ODT either with or without water and one oral dose of rivaroxaban 10 mg film-tablet. There were at least 5 days between the two doses. Observation for each participant lasted about 6 weeks in total. Blood samples were collected from the participants to measure the blood level of the study drug.


Eligibility criteria: Inclusion Criteria:

- Japanese healthy male subjects, aged 20 to 40 years (inclusive), with body mass index 17.6 to 26.4 kg/m²

Exclusion Criteria:

* Subject with 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
* Subject with known hypersensitivity to the study drugs (active substances or excipients of the preparations)
* Subject with known coagulation disorders (e.g. von Willebrand disease, hemophilia)
* Subject with febrile illness within 1 week before the first study drug administration
* Subject with suspicion of drug or alcohol abuse
* Subject with intake of foods or beverages containing grapefruit, pomelo, Seville orange, and tangelo within 1 week before the first study drug administration
* Subject with therapies (e.g. physiotherapy, acupuncture, etc.) within 1 month before starting study treatment
* Subject with clinically relevant findings in the electrocardiogram (ECG) such as a second- or third-degree atrioventricular block, prolongation of the QRS complex over 120 msec or of the corrected QT (QTc) interval over 450 msec
* Subject with systolic blood pressure below 90 or above 130 mmHg
* Subject with diastolic blood pressure below 45 or above 85 mmHg
* Subject with clinically relevant deviations of the screened laboratory parameters from reference ranges

Primary outcomes:
measure: Cmax for plasma rivaroxaban concentration
timeFrame: Up to 48 hours after study medication
measure: AUC(0-tlast) for plasma rivaroxaban concentration
timeFrame: Up to 48 hours after study medication
Secondary outcomes:
measure: Number of subjects with treatment-emergent adverse events
timeFrame: Up to 30 days after study medication
Other outcomes:
Locations:
city: Sumida-ku
country: Japan
facility: Sumida Hospital
state: Tokyo
city: Fukuoka
country: Japan
facility: Fukuoka Mirai Hospital
city: Kumamoto
country: Japan
facility: Medical Co. LTA Nishikumamoto hospital
Study officials:
References: