Bioequivalence Study of Rivaroxaban 2.5 mg Tablets Under Fasting and Fed Conditions

NCT07807488 | Completed Phase 1

• 2 other identifiers: QLS1002-01CTR20220294
• Study Type: interventional
• Target: 64
• Locations: 1 country
• Sites: 1

Brief Summary

This completed study compared how the body absorbed a single 2.5 mg dose of a test rivaroxaban tablet and the reference product (Xarelto) in healthy adults. The comparison was conducted separately under fasting and fed conditions. The study also evaluated the safety and tolerability of both products.

Conditions

Healthy Participants

Keywords

Rivaroxaban; Bioequivalence; Pharmacokinetics; Fasting; Fed

Outcome Measures

Primary Outcomes (3)

• Maximum Plasma Concentration (Cmax) of Rivaroxaban

  The maximum observed plasma concentration of rivaroxaban after administration of the test or reference formulation, reported in ng/mL.

  Predose through 48 hours after each dose

• Area Under the Plasma Concentration-Time Curve From Time Zero to the Last Quantifiable Concentration (AUC0-t)

  Area under the rivaroxaban plasma concentration-time curve from time zero to the last quantifiable concentration, calculated after administration of the test or reference formulation and reported in h\*ng/mL.

  Predose through 48 hours after each dose

• Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinity (AUC0-infinity)

  Area under the rivaroxaban plasma concentration-time curve from time zero extrapolated to infinity, calculated after administration of the test or reference formulation and reported in h\*ng/mL.

  Predose through 48 hours after each dose

Secondary Outcomes (4)

• Time to Maximum Plasma Concentration (Tmax) of Rivaroxaban

  Predose through 48 hours after each dose

• Terminal Elimination Half-Life (t1/2) of Rivaroxaban

  Predose through 48 hours after each dose

• Terminal Elimination Rate Constant (Lambda z) of Rivaroxaban

  Predose through 48 hours after each dose

• Number of Participants With Adverse Events

  From the first dose through the end-of-study safety follow-up, up to 40 days

Study Arms (2)

TRTR Sequence

OTHER

Participants received the test formulation in Periods 1 and 3 and the reference formulation in Periods 2 and 4. The same sequence was used within both the fasting and fed cohorts.

Drug: Rivaroxaban 2.5 mg Test Tablet; Drug: Rivaroxaban 2.5 mg Reference Tablet

RTRT Sequence

OTHER

Participants received the reference formulation in Periods 1 and 3 and the test formulation in Periods 2 and 4. The same sequence was used within both the fasting and fed cohorts.

Drug: Rivaroxaban 2.5 mg Test Tablet; Drug: Rivaroxaban 2.5 mg Reference Tablet

Interventions

Rivaroxaban 2.5 mg Reference Tablet DRUG

One 2.5 mg Xarelto rivaroxaban tablet manufactured by Bayer Pharma AG was administered orally with 240 mL of water in the assigned study periods.

RTRT Sequence; TRTR Sequence

Rivaroxaban 2.5 mg Test Tablet DRUG

One 2.5 mg rivaroxaban tablet manufactured by Qilu Pharmaceutical Co., Ltd. was administered orally with 240 mL of water in the assigned study periods.

RTRT Sequence; TRTR Sequence

Eligibility Criteria

• Age: 18 Years+
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Healthy male or female participant aged 18 years or older.
• Body weight at least 50 kg for males or at least 45 kg for females, with body mass index from 19.0 to 26.0 kg/m2, inclusive.
• No plan for conception or gamete donation and willing to use effective contraception from screening (from 2 weeks before screening for females) until 6 months after the last dose.
• Creatinine clearance greater than 80 mL/min.
• Prothrombin time and activated partial thromboplastin time within the normal ranges.
• Voluntarily provided written informed consent and understood the study procedures.
• Able to comply with and complete the study requirements.

You may not qualify if:

• Specific allergy history, current allergic disease, allergic constitution, or known hypersensitivity to rivaroxaban, related compounds, or formulation components.
• Clinically significant abnormal findings on physical examination, vital signs, electrocardiogram, or clinical laboratory testing.
• Clinically significant neurologic, cardiovascular, renal, hepatic, gastrointestinal, respiratory, metabolic, musculoskeletal, or other disease that could affect drug absorption, distribution, metabolism, or excretion.
• Active pathological bleeding, coagulation abnormality, or clinically relevant bleeding risk.
• Positive test for human immunodeficiency virus antibody, hepatitis B surface antigen, hepatitis C antibody, or syphilis antibody.
• Hereditary lactose or galactose intolerance, total lactase deficiency, or glucose-galactose malabsorption.
• Positive pregnancy test or breastfeeding.
• History of drug abuse within 5 years or positive urine drug screen.
• Hospitalization or surgery within 3 months before screening.
• Regular alcohol intake exceeding 14 units per week within 3 months or positive breath alcohol test.
• Smoking more than 5 cigarettes per day on average within 3 months.
• Participation in another clinical study with study drug exposure within 3 months.
• Blood donation or blood loss of at least 400 mL within 3 months, or donation of 2 therapeutic units of platelets within 1 month.
• Use of prescription medication within 14 days, or nonprescription medication, herbal medicine, or health products within 7 days before dosing.
• Use within 28 days before first dosing of drugs that strongly inhibit or induce P-glycoprotein or CYP3A4.

Sponsors & Collaborators

• The Affiliated Hospital of Qingdao University: lead

Study Sites (1)

The Affiliated Hospital of Qingdao University

Qingdao, Shandong, China

Location

MeSH Terms

Conditions

Fasting; Lecithin Cholesterol Acyltransferase Deficiency

Interventions

Rivaroxaban

Condition Hierarchy (Ancestors)

Feeding Behavior; Behavior; Hypoalphalipoproteinemias; Hypolipoproteinemias; Lipid Metabolism, Inborn Errors; Metabolism, Inborn Errors; Genetic Diseases, Inborn; Congenital, Hereditary, and Neonatal Diseases and Abnormalities; Dyslipidemias; Lipid Metabolism Disorders; Metabolic Diseases; Nutritional and Metabolic Diseases

Intervention Hierarchy (Ancestors)

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

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: OTHER
• Responsible Party: PRINCIPAL INVESTIGATOR
• PI Title: Principal Investigator

Model Details: Two independently enrolled cohorts (fasting and fed) were evaluated separately. Within each cohort, participants were randomized 1:1 to one of two fully replicated four-period sequences: TRTR or RTRT.

Study Record Dates

• First Submitted: September 2, 2026
• First Posted: September 8, 2026
• Study Start: March 16, 2022
• Primary Completion: April 15, 2022
• Study Completion: April 25, 2022
• Last Updated: September 8, 2026

Record last verified: 2026-09

Locations

CN (1)