Healthy SubjectsPhase 1NCT02882425
Absolute Bioavailability of a Single Oral Dose of Selexipag in Healthy Subjects
A Phase 1 study testing Selexipag for intravenous use and Selexipag for oral use in people with Healthy Subjects, run by Actelion.
Trial summary
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. Read more about this study
- Who is it for?
- Ages 18 to 45 years, men onlyHealthy volunteers can take part
- Conditions the study is for
- Healthy Subjects
- What is being tested?
- Selexipag for intravenous use and Selexipag for oral use
- Type of treatment
- Pill or oral medicine, Injection or infusion
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 19 participants
- Where
- No sites listed yet
- Study dates
- Jan 2015to Apr 2015
- Phase
- Phase 1
- Are there results?
- None posted in the registry
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 45 years
- Men only
- Healthy volunteers accepted
- Adult
Who may be able to join
- 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
Who cannot join
- 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
About this study
Official 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
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.
Read the detailed description
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.
- Conditions
- Healthy Subjects
- Being tested
- Selexipag for intravenous use, Selexipag for oral use
- Keywords
- selexipag, bioavailability
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
Selexipag for intravenous useDrug
Also called ACT-293987
Selexipag was reconstituted in sterile 0.9% w/v NaCl before infusion via an infusion pump at a rate of 2.5 µg/min.
Selexipag for oral useDrug
Also called ACT-293987
Tablet containing 200 µg of selexipag
| Study group | Role | What they receive |
|---|---|---|
| Intravenous selexipag (Pilot phase) | Experimental | Subjects received a 20-minute intravenous (i.v.) infusion of 50 µg selexipag Receives: Drug: Selexipag for intravenous use |
| Sequence A-B (Main phase) | Experimental | Subjects received a 80-minute i.v. infusion of 200 µg selexipag during Period 1, and 2 tablets of oral selexipag (total dose of 400 µg) as a single administration during Period 2. A washout period of 7 to 10 days separated the i.v. infusion from the oral administration. Receives: Drug: Selexipag for intravenous use; Drug: Selexipag for oral use |
| Sequence B-A (Main phase) | Experimental | Subjects received 2 tablets of oral selexipag (total dose of 400 µg) as a single administration during Period 1, and a 80-minute i.v. infusion of 200 µg selexipag during Period 2. A washout period of 7 to 10 days separated the oral administration from the i.v. infusion. Receives: Drug: Selexipag for intravenous use; Drug: Selexipag for oral use |
What is being measured
The primary outcome is the main question the study is designed to answer.
Absolute bioavailability (F) of selexipag
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
Measured: From pre-dose to 72 hours post-dose
Area under the plasma concentration-time curve from time 0 to infinity [AUC(0-inf)] of selexipag
AUC(0-inf) was calculated from the concentration-time profile of selexipag after both oral and intravenous administration during the main phase
Measured: From pre-dose to 72 hours post-dose
Secondary outcomes (5)
Areas under the plasma concentration-time curve from time 0 to time t [AUC(0-t)] of selexipag and its active metabolite
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
Measured: From pre-dose to 72 hours post-dose
Maximum plasma concentration (Cmax) of selexipag and its active metabolite
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
Measured: From pre-dose to 72 hours post-dose
time to reach maximum plasma concentration (tmax) of selexipag and its active metabolite
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
Measured: From pre-dose to 72 hours post-dose
Terminal half-life [t(1/2)] of selexipag and its active metabolite
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
Measured: From pre-dose to 72 hours post-dose
Number of participants experiencing Adverse Events (AEs) and Serious Adverse Events (SAEs)
Measured: 4 days
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted29 Aug 2016 (estimated)
- Study startJan 2015
- Primary completionApr 2015
- Study completionApr 2015
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Publications (1)Papers the sponsor has linked to this study.
- Other trials for Healthy SubjectsStudies of the same condition, open and under way.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Other
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Enrolment
- 19 participants (actual)
Sponsor and investigators
- Lead sponsor
- Actelion
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
- Investigators
- Priska Kaufmann, PhD, Study director, Actelion
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT02882425
- Sponsor's protocol ID
- AC-065-110
- Status last verified
- Jan 2025
- First submitted
- 18 Aug 2016
- Last updated
- 3 Feb 2025
- Results posted
- No
- Data monitoring committee
- No
Publications
Kaufmann P, Hurst N, Astruc B, Dingemanse J. Absolute oral bioavailability of selexipag, a novel oral prostacyclin IP receptor agonist. Eur J Clin Pharmacol. 2017 Feb;73(2):151-156. doi: 10.1007/s00228-016-2164-4. Epub 2016 Nov 24.
PubMed 27885399
Study at a glance
From the registry record, last updated by the sponsor on 3 Feb 2025. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official 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
- ClinicalTrials.gov ID
- NCT02882425
- Acronym / sponsor ID
- AC-065-110
- Conditions
- Healthy Subjects
- Keywords
- selexipag, bioavailability
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 19 participants (actual)
- Lead sponsor
- ActelionIndustry (pharma, biotech, devices)
- Study start
- Jan 2015
- Primary completion
- Apr 2015 (actual)
- Study completion
- Apr 2015 (actual)
- First posted
- 29 Aug 2016 (estimated)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
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.
Detailed description
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.
Study design
- Primary purpose
- Other
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Number of arms
- 3
| Arm | Type | Receives |
|---|---|---|
| Intravenous selexipag (Pilot phase) | Experimental | Drug: Selexipag for intravenous useSubjects received a 20-minute intravenous (i.v.) infusion of 50 µg selexipag |
| Sequence A-B (Main phase) | Experimental | Drug: Selexipag for intravenous use, Drug: Selexipag for oral useSubjects received a 80-minute i.v. infusion of 200 µg selexipag during Period 1, and 2 tablets of oral selexipag (total dose of 400 µg) as a single administration during Period 2. A washout period of 7 to 10 days separated the i.v. infusion from the oral administration. |
| Sequence B-A (Main phase) | Experimental | Drug: Selexipag for intravenous use, Drug: Selexipag for oral useSubjects received 2 tablets of oral selexipag (total dose of 400 µg) as a single administration during Period 1, and a 80-minute i.v. infusion of 200 µg selexipag during Period 2. A washout period of 7 to 10 days separated the oral administration from the i.v. infusion. |
Who may qualify
- Ages
- 18 to 45 years
- Sex
- Male only
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (4 listed)
- 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
Key exclusion criteria (3 listed)
- 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
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| Selexipag for intravenous useAlso: ACT-293987Selexipag was reconstituted in sterile 0.9% w/v NaCl before infusion via an infusion pump at a rate of 2.5 µg/min. | Drug | Intravenous selexipag (Pilot phase), Sequence A-B (Main phase), Sequence B-A (Main phase) |
| Selexipag for oral useAlso: ACT-293987Tablet containing 200 µg of selexipag | Drug | Sequence A-B (Main phase), Sequence B-A (Main phase) |
Primary outcome
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
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
5 secondary outcomes
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
Maximum plasma concentration (Cmax) of selexipag and its active metabolite
Time frame: From pre-dose to 72 hours post-dose
time to reach maximum plasma concentration (tmax) of selexipag and its active metabolite
Time frame: From pre-dose to 72 hours post-dose
Terminal half-life [t(1/2)] of selexipag and its active metabolite
Time frame: From pre-dose to 72 hours post-dose
Number of participants experiencing Adverse Events (AEs) and Serious Adverse Events (SAEs)
Time frame: 4 days
Results and safety
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 3 Feb 2025.
- Results publication: PubMed 27885399Kaufmann P, Hurst N, Astruc B, Dingemanse J. Absolute oral bioavailability of selexipag, a novel oral prostacyclin IP receptor agonist. Eur J Clin Pharmacol. 2017 Feb;73(2):151-156. doi: 10.1007/s00228-016-2164-4. Epub 2016 Nov 24.
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Priska Kaufmann, PhD study director
Actelion
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing Selexipag for intravenous use and Selexipag for oral use in people with Healthy Subjects, run by Actelion.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 4 inclusion and 3 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 3 Feb 2025. Status can change between updates, so confirm with the study contact before making plans.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Absolute bioavailability (F) of selexipag (time frame: From pre-dose to 72 hours post-dose). The study lists 2 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
On the ClinicalTrials.gov record for NCT02882425, which also lists 1 linked publication.
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 3 Feb 2025.