Bioequivalence Study of Bosentan 125 mg Tablets Immediate Release (IR) Versus Tracleer® 125 mg Tablets IR In Healthy Subjects

Two-way Crossover, Open-label, Single-dose, Bioequivalence Study of Bosentan (LLC "GEROPHARM", Russia) 125 mg Tablets Immediate Release (IR )Versus Tracleer® (Actelion Pharmaceuticals Ltd., Switzerland) 125 mg Tablets IR in Normal Healthy Subjects Under Fasting Conditions

Bioequivalence Study of 2 formulation of bosentan (Bosentan GEROPHARM vers. Tracleer® Actelion)

Study Overview

• Status: Completed
• Conditions: Bioequivalence
• Intervention / Treatment: Drug: Bosentan 125 mg; Drug: Tracleer 125Mg Tablet

Detailed Description

Study to evaluate the bioequivalence of orally administered bosentan preparations, immediate release tablets, 125 mg in normal healthy subjects under fasting conditions

• Study Type: Interventional
• Enrollment (Actual): 64
• Phase: Phase 1

Contacts and Locations

Study Locations

• Russian Federation
  • Yaroslavl, Russian Federation, 150007
    • Clinical Hospital № 3

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 14 years to 41 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Signed informed consent form.
• Healthy male aged 18 to 45 years.
• Verified diagnosis is "healthy" according to data Standard clinical, laboratory and Instrumental methods of examination.
• Have a body mass index between 18,5 and 30 kg/m2.
• Subjects must use, with their partner, methods of highly effective contraception throughout the study and 30 days after the end of study.
• Ability to keep fasting state for at least 14 hours.
• Consent and ability to respect the schedule of visits and the points of the Protocol.

Exclusion Criteria:

• History of serious allergic problems/events.
• Medicinal intolerance.
• Any acute and chronic diseases of the cardiovascular system, cardiovascular, bronchopulmonary, neuroendocrine systems, as well as diseases of the gastrointestinal tract, liver, kidneys, blood.
• Psychiatric disorders, history of epilepsy and seizures.
• Acute infectious diseases in less than 4 weeks before the start of the study.
• Subjects who have taken medication 2 weeks preceding before the study.
• Subjects who have taken any drugs known effects on hemodynamics or to induce or inhibit hepatic drug metabolism within 30 days prior to administration of the study medication (examples of inducers: barbiturates, omeprazole, etc.).
• Donation of plasma (450 mL or more) within 2 month prior to administration of the study medication.
• History of significant alcohol or drugs abuse or any indication of the regular use of more than 10 units of alcohol per week (1 Unit = 200 mL of wine or 500 mL of beer or 50 mL of alcohol 40%).
• Smokers.
• Participation in other clinical training is less than than for 3 months before the study.
• Lack of signed informed consent form.
• 10% deviation from references in lab tests.
• Positive testing for alcohol, drugs.
• Dehydration due to diarrhea, vomiting, or other causes within the last 24 hours before the start of the study.
• Any diet (vegetarian, etc.) extreme physical exercise, night shift work.
• Heart rate below 60 or above 80 beats per minute.
• Systolic blood pressure less than 110 mm Hg or more than 139 mm Hg.
• Diastolic blood pressure less than 60 mm Hg or more than 89 mm Hg.
• Volunteers, for Investigator opinion, who can not understand and evaluate the information about this study.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Bosentan; Single administered dose of Bosentan (125 mg tablet immediate release) in a fasting condition	Drug: Bosentan 125 mg; Single administered dose of Bosentan (125 mg tablet immediate release) in a fasting condition; Other Names: bosentan
Active Comparator: Tracleer®; Single administered dose of Tracleer® (125 mg tablet immediate release) in a fasting condition	Drug: Tracleer 125Mg Tablet; Single administered dose of Tracleer® (125 mg tablet immediate release) in a fasting condition; Other Names: bosentan

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cmax	Pharmacokinetics of bosentan by Assessment of Observed Maximum Plasma Concentration (Cmax)	0 hours (pre-dose), as well as at 0.5, 1, 1.5, 2, 2.5, 3, 3,5, 3,75, 4, 4.25, 4.5, 4.75, 5, 6, 8, 10, 12, 14 and 24 hour post-dose.
AUC(0-t)	Pharmacokinetics of bosentan by Assessment of Area Under the Curve From Time Zero Extrapolated to "t" (AUC(0-t))	0 hours (pre-dose), as well as at 0.5, 1, 1.5, 2, 2.5, 3, 3,5, 3,75, 4, 4.25, 4.5, 4.75, 5, 6, 8, 10, 12, 14 and 24 hour post-dose.

Collaborators and Investigators

• Sponsor: Geropharm

Study record dates

Study Major Dates

• Study Start (Actual): May 24, 2018
• Primary Completion (Actual): June 20, 2018
• Study Completion (Actual): June 20, 2018

Study Registration Dates

• First Submitted: September 23, 2019
• First Submitted That Met QC Criteria: September 23, 2019
• First Posted (Actual): September 24, 2019

Study Record Updates

• Last Update Posted (Actual): September 24, 2019
• Last Update Submitted That Met QC Criteria: September 23, 2019
• Last Verified: March 1, 2019

More Information

Terms related to this study

• Keywords: Pharmacokinetics; fasting; AUC; Cmax; bosentan
• Additional Relevant MeSH Terms: Molecular Mechanisms of Pharmacological Action; Antihypertensive Agents; Endothelin Receptor Antagonists; Bosentan
• Other Study ID Numbers: BOZ-501

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: No

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No