A Clinical Study to Assess the Effect of Clopidogrel on the Pharmacokinetics of Selexipag and Its Active Metabolite in Healthy Male Subjects

NCT ID: NCT03496506

Last Updated: 2025-06-22

Basic Information

• Recruitment Status: COMPLETED
• Clinical Phase: PHASE1
• Total Enrollment: 22 participants
• Study Classification: INTERVENTIONAL
• Study Start Date: 2018-03-05
• Study Completion Date: 2018-05-18

Brief Summary

The purpose of this study is to evaluate the effect of clopidogrel on the pharmacokinetics of selexipag and its active metabolite (ACT-333679) in healthy male adults (by determining the blood concentrations of selexipag and its metabolite). Also, the safety of selexipag when administered alone or with clopidogrel will be assessed.

Conditions

Healthy Subjects

Study Design

• Allocation Method: NA
• Intervention Model: SINGLE_GROUP
• Primary Study Purpose: OTHER
• Blinding Strategy: NONE

Study Groups

Sequential treatment arm

Subjects receive 1 tablet of selexipag twice daily from Day 1 to Day 9 and 1 tablet in the morning of Day 10. In the morning of Day 4 and 1 hour before the administration of selexipag, they receive 4 tablets of clopidogrel. Then from Day 5 to Day 10, 1 hour before the morning administration of selexipag, they receive 1 tablet of clopidogrel .

Group Type: EXPERIMENTAL

Selexipag

Intervention Type: DRUG

Each film-coated tablet contains 200 microgram (mcg) of selexipag (oral use)

Clopidogrel

Intervention Type: DRUG

Each film-coated tablet containing 75 mg of clopidogrel (oral use)

Interventions

Selexipag

Each film-coated tablet contains 200 microgram (mcg) of selexipag (oral use)

Intervention Type: DRUG

Clopidogrel

Each film-coated tablet containing 75 mg of clopidogrel (oral use)

Intervention Type: DRUG

Other Intervention Names

ACT-293987

Eligibility Criteria

Inclusion Criteria

• Signed informed consent in the local language prior to any study-mandated procedure.
• Healty male subjects aged between 18 and 45 years (inclusive) at screening.
• Body mass index from 18.0 to 28.0 kg/m2 (inclusive) at screening.
• Systolic blood pressure (SBP) 100-145 mmHg, diastolic blood pressure (DBP) 50-90 mmHg, and pulse rate 45-90 bpm (inclusive).

Exclusion Criteria

• Any contraindication included in the SmPC of selexipag or clopidogrel treatment.
• History or clinical evidence of any disease and/or existence of any surgical or medical condition, which might interfere with the absorption, distribution, metabolism or excretion of the study treatments.
• History or clinical evidence of any disorder of hemostasis, hemorrhagic diathesis, nose or gingival bleeding, hemophilia, thrombotic thrombocytopenic purpura, presence of any lesions with a propensity to bleed (particularly gastrointestinal and intraocular), history of bleeding complications after surgical procedures such as tooth extraction
• Previous history of stroke, fainting, collapse, syncope, orthostatic hypotension,vasovagal reactions, head injury.
• Excessive caffeine consumption
• Nicotine consumption within 3 months prior to screening, and inability to refrain from nicotine consumption during the course of the study
• Previous treatment with any prescribed medications (including vaccines) or over the counter (OTC) medications (including herbal medicines such as St John's Wort, homeopathic preparations, vitamins, and minerals) within 2 weeks prior to first selexipag administration.
• Subjects with rare hereditary problems of galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption.
• Any circumstances or conditions, which, in the opinion of the investigator, may affect the subject's full participation in the study or compliance with the protocol.

• Minimum Eligible Age: 18 Years
• Maximum Eligible Age: 45 Years
• Eligible Sex: MALE
• Accepts Healthy Volunteers: Yes

Sponsors

Actelion

INDUSTRY

Sponsor Role: lead

Responsible Party

Responsibility Role: SPONSOR

Principal Investigators

Shirin Bruderer

Role: STUDY_DIRECTOR

Actelion

Locations

Clinical Pharmacology Unit (CPU)

Merksem, , Belgium

Countries

Belgium

References

Axelsen LN, Poggesi I, Rasschaert F, Perez Ruixo JJ, Bruderer S. Clopidogrel, a CYP2C8 inhibitor, causes a clinically relevant increase in the systemic exposure to the active metabolite of selexipag in healthy subjects. Br J Clin Pharmacol. 2021 Jan;87(1):119-128. doi: 10.1111/bcp.14365. Epub 2020 Jun 5.

Reference Type: DERIVED

PMID: 32415684 (View on PubMed)

Other Identifiers

AC-065-117

Identifier Type: -

Identifier Source: org_study_id