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Completed

NCT Number: NCT02882425

Absolute Bioavailability of a Single Oral Dose of Selexipag in Healthy Subjects

The primary purpose of this phase 1 study is to investigate the absolute bio-availability of a single oral dose of selexipag, i.e., to assess the amount of selexipag which reaches the blood when administered as an oral tablet (ACT-293987) compared to an intravenous administration in healthy subjects.

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Key information

Conditions

Healthy Subjects

Age range

18 year–45 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

About this study

A pilot phase was conducted in 3 male subjects before the main phase for assessment of absolute bio-availability conducted in 16 other male subjects. The pilot phase aimed to determine the intravenous dose to be used in the main phase based on safety data and pharmacokinetics data.

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • Signed informed consent prior to any study-mandated procedure
  • Aged from 18 to 45 (inclusive) at screening
  • Body mass index (BMI) from 18.0 to 28.0 kg/m2 (inclusive) at screening
  • Healthy on the basis of physical examination, cardiovascular assessments and laboratory tests

Exclusion criteria

  • Any contraindication to the study drug formulations
  • History or presence of any disease or 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 drugs
  • 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

Treatment and study plan

Selexipag for intravenous use

Drug

Selexipag was reconstituted in sterile 0.9% w/v NaCl before infusion via an infusion pump at a rate of 2.5 µg/min.

Other names: ACT-293987

Selexipag for oral use

Drug

Tablet containing 200 µg of selexipag

Other names: ACT-293987

Primary outcomes

  1. Absolute bioavailability (F) of selexipag

    Time frame: From pre-dose to 72 hours post-dose

    F was calculated using the areas under the plasma concentrations curves extrapolated to infinity [AUC(0-inf)] after oral (po) and intravenous (iv) doses, obtained during the main phase, and using the following formula: AUC(0-inf)po * iv dose / AUC(0-inf)iv * oral dose

  2. Area under the plasma concentration-time curve from time 0 to infinity [AUC(0-inf)] of selexipag

    Time frame: From pre-dose to 72 hours post-dose

    AUC(0-inf) was calculated from the concentration-time profile of selexipag after both oral and intravenous administration during the main phase

Secondary outcomes

  1. Areas under the plasma concentration-time curve from time 0 to time t [AUC(0-t)] of selexipag and its active metabolite

    Time frame: From pre-dose to 72 hours post-dose

    AUC from time 0 to time t of the last measured concentration above the limit of quantification [AUC(0-t)] were calculated for selexipag and its active metabolite, from their respective concentration-time profiles, after both intravenous (pilot phase and main phase) and oral administration (main phase) of selexipag

  2. Maximum plasma concentration (Cmax) of selexipag and its active metabolite

    Time frame: From pre-dose to 72 hours post-dose

    Cmax of selexipag and its active metabolite were directly obtained from the plasma concentration-time curves after both intravenous (pilot phase and main phase) and oral administration (main phase) of selexipag

  3. time to reach maximum plasma concentration (tmax) of selexipag and its active metabolite

    Time frame: From pre-dose to 72 hours post-dose

    tmax of selexipag and its active metabolite were directly obtained from the plasma concentration-time curves after both intravenous (pilot phase and main phase) and oral administration (main phase) of selexipag

  4. Terminal half-life [t(1/2)] of selexipag and its active metabolite

    Time frame: From pre-dose to 72 hours post-dose

    t(1/2) of selexipag and its active metabolite were calculated after both intravenous (pilot phase and main phase) and oral administration (main phase) of selexipag from the concentration-time profiles

  5. Number of participants experiencing Adverse Events (AEs) and Serious Adverse Events (SAEs)

    Time frame: 4 days

Sponsors and collaborators

Lead sponsor

Actelion

Industry

Registry information

Official study title

Single-center, Open-label, Phase 1 Study Consisting of a Single-dose Pilot Phase and a Randomized, Two-way Crossover, Single-dose Main Phase to Investigate the Absolute Bioavailability of a Single Oral Dose of Selexipag in Healthy Male Subjects

Important dates

Study start
2015
Primary completion
2015
Study completion
2015
First posted
Aug 29, 2016
Registry last updated
Feb 3, 2025

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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