Clinical trial NCT02882425: Absolute Bioavailability of a Single Oral Dose of Selexipag in Healthy Subjects
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
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy Subjects
Keywords: selexipag
bioavailability
Lead sponsor: Actelion
Sponsor class: INDUSTRY
First posted: 2016-08-29
Enrollment: 19
Sex: MALE
Minimum age (years): 18
Maximum age (years): 45
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: CROSSOVER
Primary purpose: OTHER

Brief 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.

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.

Eligibility criteria: 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

Primary outcomes:
measure: Absolute bioavailability (F) of selexipag
timeFrame: From pre-dose to 72 hours post-dose
measure: Area under the plasma concentration-time curve from time 0 to infinity [AUC(0-inf)] of selexipag
timeFrame: From pre-dose to 72 hours post-dose
Secondary outcomes:
measure: Areas under the plasma concentration-time curve from time 0 to time t [AUC(0-t)] of selexipag and its active metabolite
timeFrame: From pre-dose to 72 hours post-dose
measure: Maximum plasma concentration (Cmax) of selexipag and its active metabolite
timeFrame: From pre-dose to 72 hours post-dose
measure: time to reach maximum plasma concentration (tmax) of selexipag and its active metabolite
timeFrame: From pre-dose to 72 hours post-dose
measure: Terminal half-life [t(1/2)] of selexipag and its active metabolite
timeFrame: From pre-dose to 72 hours post-dose
measure: Number of participants experiencing Adverse Events (AEs) and Serious Adverse Events (SAEs)
timeFrame: 4 days
Other outcomes:
Locations:
Study officials:
affiliation: Actelion
name: Priska Kaufmann, PhD
role: STUDY_DIRECTOR
References:
citation: 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.