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

NCT02882425 | Completed Phase 1

• 1 other identifier: AC-065-110
• Study Type: interventional
• Target: 19
• Locations: 0 countries
• Sites: N/A

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.

Conditions

Healthy Subjects

Keywords

selexipag; bioavailability

Outcome Measures

Primary Outcomes (2)

• 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

  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

  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

  From pre-dose to 72 hours post-dose

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

  From pre-dose to 72 hours post-dose

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

  From pre-dose to 72 hours post-dose

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

  From pre-dose to 72 hours post-dose

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

  4 days

Study Arms (3)

Intravenous selexipag (Pilot phase)

EXPERIMENTAL

Subjects received a 20-minute intravenous (i.v.) infusion of 50 µg selexipag

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.

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.

Drug: Selexipag for intravenous use; Drug: Selexipag for oral use

Interventions

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.

Also known as: ACT-293987

Intravenous selexipag (Pilot phase); Sequence A-B (Main phase); Sequence B-A (Main phase)

Selexipag for oral use DRUG

Tablet containing 200 µg of selexipag

Also known as: ACT-293987

Sequence A-B (Main phase); Sequence B-A (Main phase)

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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

Sponsors & Collaborators

• Actelion: lead

Related Publications (1)

• 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.

  PMID: 27885399 RESULT

MeSH Terms

Interventions

selexipag

Study Officials

• Priska Kaufmann, PhD

  Actelion

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: August 18, 2016
• First Posted: August 29, 2016
• Study Start: January 1, 2015
• Primary Completion: April 1, 2015
• Study Completion: April 1, 2015
• Last Updated: February 3, 2025

Record last verified: 2025-01