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

Actelion Pharmaceuticals

Status and phase: Completed; Phase 1

Conditions: Healthy Subjects

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

Study type: Interventional

Funder types: Industry

Identifiers

NCT02882425

AC-065-110

Details and patient eligibility

About

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.

Full 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.

Enrollment: 19 patients

Sex: Male

Ages: 18 to 45 years old

Volunteers: Accepts Healthy Volunteers

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

Trial design

Primary purpose: Other

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

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19 participants in 3 patient groups

Intravenous selexipag (Pilot phase)

Experimental group

Description:

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

Treatment:

Drug: Selexipag for intravenous use

Sequence A-B (Main phase)

Experimental group

Description:

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.

Treatment:

Drug: Selexipag for intravenous use

Drug: Selexipag for oral use

Sequence B-A (Main phase)

Experimental group

Description:

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.

Treatment:

Drug: Selexipag for intravenous use

Drug: Selexipag for oral use