Comparison of Two Dose Strengths of Selexipag in Healthy Adults

Single-center, Open-label, Randomized, Two-way Crossover Study in Healthy Adult Male Subjects to Compare the Pharmacokinetics of Selexipag (ACT-293987) Following Single Oral Administration of 4 Film-coated Pediatric Tablets of 50 µg vs One Film-coated Tablet of 200 µg Selexipag

Clinical study in healthy adult subjects to compare the adult tablet of selexipag with the tablet developed for children.

Study Overview

• Status: Completed
• Conditions: Healthy Subjects
• Intervention / Treatment: Drug: Selexipag (adult formulation); Drug: Selexipag (pediatric formulation)

Detailed Description

Healthy male adults receive a single dose of selexipag (200 µg) but using a different tablet strength (4 film-coated pediatric tablets of 50 µg versus one film-coated tablet of 200 µg selexipag) during each of the two study periods. There is a washout of 7-9 days between the two study treatment administrations.

• Study Type: Interventional
• Enrollment (Actual): 20
• Phase: Phase 1

Contacts and Locations

Study Locations

• Germany
  • Kiel, Germany, 24105
    • Investigator Site.

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (Adult)
• Accepts Healthy Volunteers: Yes

Description

Key inclusion Criteria:

• Male subjects aged from 18 to 45 years (inclusive) at screening
• Signed informed consent form
• Body mass index (BMI) between 18.0 and 28.0 kg/m2 (inclusive) at screening
• Healthy on the basis of physical examination,cardiovascular assessments and laboratory tests

Key exclusion Criteria:

• Any contraindication to the study treatments
• History or clinical evidence of any disease or medical / surgical condition or treatment, which may put the subject at risk of participation in the study or may interfere with the absorption, distribution, metabolism or excretion of the study treatments
• 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

Study Plan

How is the study designed?

Design Details

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

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Sequence AB; Subjects receive 200 µg of selexipag (adult formulation) as a single oral dose during Period 1 and 200 µg of selexipag (pediatric formulation) as a single oral dose during Period 2	Drug: Selexipag (adult formulation); One selexipag film-coated tablet of 200 µg; Other Names: ACT-293987; Drug: Selexipag (pediatric formulation); Four selexipag film-coated tablets of 50 µg; Other Names: ACT-293987
Experimental: Sequence BA; Subjects receive 200 µg of selexipag (pediatric formulation) as a single oral dose during Period 1 and 200 µg of selexipag (adult formulation) as a single oral dose during Period 2	Drug: Selexipag (adult formulation); One selexipag film-coated tablet of 200 µg; Other Names: ACT-293987; Drug: Selexipag (pediatric formulation); Four selexipag film-coated tablets of 50 µg; Other Names: ACT-293987

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Area under plasma concentration-time curve [AUC(0-inf)] of selexipag and ACT-333679	AUC(0-inf) is the area under plasma concentration-time curves for selexipag and its metabolite (ACT-333679), calculated from zero to the extrapolated infinite time	From predose until 72 hours postdose for each treatment period
Maximum plasma concentration (Cmax) of selexipag and ACT-333679	Cmax is directly derived from the individual plasma concentration time curves for selexipag and its metabolite ACT-333679	From predose until 72 hours postdose for each treatment period

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Time to reach Cmax (tmax) of selexipag and ACT-333679	tmax is directly derived from the individual plasma concentration time curves for selexipag and its metabolite ACT-333679	From predose until 72 hours postdose for each treatment period
Terminal half-life (t½) of selexipag and ACT-333679	The period of time required for the concentration levels of selexipag or its metabolite (ACT-333679) to be reduced by one-half	From predose until 72 hours postdose for each treatment period
Area under plasma concentration-time curve [AUC(0-t)] of selexipag and ACT-333679	AUC(0-t) is the area under plasma concentration-time curves for selexipag and its metabolite (ACT-333679), calculated from zero to time t of the last measured concentration above the limit of quantification	From predose until 72 hours postdose for each treatment period
Incidence of treatment-emergent adverse events and serious adverse events	A treatment-emergent AE is any AE temporally associated with the use of a study treatment, whether or not considered related to the study treatment, including any abnormalities in ECG parameters, vital signs or laboratory tests	From first administration of selexipag (Day 1 Period 1) to end of study (Day 4, Period 2)
Incidence of safety events of interest	Events of interest include any abnormalities in ECG, vital signs or laboratory test results	From first administration of selexipag (Day 1 Period 1) to end of study (Day 4, Period 2)

Collaborators and Investigators

• Sponsor: Actelion
• Investigators: Margaux Boehler, Actelion

Publications and helpful links

General Publications

• Boehler M, Bruderer S, Ulc I, Dingemanse J. Biocomparison Study of Adult and Paediatric Dose Strengths of the Prostacyclin Receptor Agonist Selexipag. Eur J Drug Metab Pharmacokinet. 2018 Feb;43(1):115-120. doi: 10.1007/s13318-017-0424-z.

Study record dates

Study Major Dates

• Study Start: June 1, 2016
• Primary Completion (Actual): June 1, 2016
• Study Completion (Actual): June 1, 2016

Study Registration Dates

• First Submitted: April 18, 2016
• First Submitted That Met QC Criteria: April 18, 2016
• First Posted (Estimated): April 20, 2016

Study Record Updates

• Last Update Posted (Actual): March 25, 2025
• Last Update Submitted That Met QC Criteria: January 31, 2025
• Last Verified: January 1, 2025

More Information

Terms related to this study

• Keywords: pharmacokinetics; selexipag
• Additional Relevant MeSH Terms: Antihypertensive Agents; Selexipag
• Other Study ID Numbers: AC-065-112

Plan for Individual participant data (IPD)

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