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Completed

NCT Number: NCT02770222

A Clinical Study to Investigate the Effect of Gemfibrozil or Rifampicin on Blood Concentrations of Selexipag in Healthy Subjects

The primary objectives of this 2-part drug interaction study are as follows:

* To evaluate the effect of gemfibrozil on the pharmacokinetics (i.e., amount in the blood) of selexipag and its metabolite ACT-333679 (Part I). * To evaluate the effect of rifampicin on the pharmacokinetics of selexipag and its metabolite ACT-333679 (Part II).

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Key information

Conditions

Healthy Subjects

Age range

18 year–55 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

About this study

Because non-clinical studies have shown that selexipag and its active metabolite, ACT-333679, are substrates for cytochrome P450 2C8 (CYP2C8), the present clinical study aims at investigating the effect of a strong inhibitor (gemfibrozil) and a moderate inducer (rifampicin) of CYP2C8 on the pharmacokinetic of selexipag and ACT-333679 as recommended by the FDA's Guidance for Industry Drug Interaction Studies (FDA, 2012).

Who can participate

Healthy volunteers accepted: Yes

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

Inclusion criteria

  • Signed informed consent form.
  • Male subjects aged between 18 and 55 years (inclusive) at screening.
  • Body mass index of 18.0 to 28.0 kg/m2 (inclusive) at screening.
  • Healthy on the basis of physical examination, cardiovascular assessments and laboratory tests at screening.

Exclusion criteria

  • Any contraindication to gemfibrozil or rifampicin treatment.
  • History or clinical evidence of any disease and/or existence of any surgical or medical condition, which might put the subject at risk of participation in the study or interfere with the absorption, distribution, metabolism or excretion of the study treatments.
  • Any circumstances or conditions, which, in the opinion of the investigator, may affect full participation in the study or compliance with the protocol.

Treatment and study plan

Selexipag

Drug

Two selexipag film-coated tablets of 200 µg as single oral dose (total dose = 400 µg)

Other names: ACT-293987

Gemfibrozil

Drug

Gemfibrozil film-coated tablet of 600 mg administered orally b.i.d. from Day 1 to Day 9

rifampicin

Drug

Rifampicin film-coated tablet of 600 mg administered orally o.d.from Day 1 to Day 9

Primary outcomes

  1. Area under the plasma concentration-time curve from zero to infinity [AUC(0-inf)] of selexipag and ACT-333679

    Time frame: Blood samples at different time points from pre-dose up to 72 hours after selexipag administration in each study period (except for the period with co-administration of gemfibrozil: up to 144 hours)

    AUC(0-inf) is calculated for selexipag and its metabolite, ACT-333679, following administration of selexipag alone or concomitantly with gemfibrozil (Part I) or rifampicin (Part II)

  2. Maximum plasma concentration (Cmax) of selexipag and ACT-333679

    Time frame: Blood samples at different time points from pre-dose up to 72 hours after selexipag administration in each study period (except for the period with co-administration of gemfibrozil: up to 144 hours)

    Cmax is directly derived from the individual plasma concentration-time curves for selexipag and its metabolite, ACT-333679, following administration of selexipag alone or concomitantly with gemfibrozil (Part I) or rifampicin (Part II)

Secondary outcomes

  1. Area under the plasma concentration-time curve from zero to time t of the last measured concentration above the limit of quantification [(AUC(0-t)] of selexipag and ACT-333679

    Time frame: Blood samples at different time points from pre-dose up to 72 hours after selexipag administration in each study period (except for the period with co-administration of gemfibrozil: up to 144 hours)

    AUC(0-t) is calculated for selexipag and ACT-333679,following administration of selexipag alone or concomitantly with gemfibrozil (Part I) or rifampicin (Part II)

  2. Time to reach maximum plasma concentration (tmax) of selexipag and ACT-333679

    Time frame: Blood samples at different time points from pre-dose up to 72 hours after selexipag administration in each study period (except for the period with co-administration of gemfibrozil: up to 144 hours)

    tmax is directly derived from the individual plasma concentration-time curves for selexipag and its metabolite, ACT-333679, following administration of selexipag alone or concomitantly with gemfibrozil (Part I) or rifampicin (Part II)

  3. Terminal elimination half-life (t1/2) of selexipag and ACT-333679

    Time frame: Blood samples at different time points from pre-dose up to 72 hours after selexipag administration in each study period (except for the period with co-administration of gemfibrozil: up to 144 hours)

    t1/2 is the period of time required for the concentration levels of selexipag or ACT-333679 to be reduced by one-half, following administration of selexipag alone or concomitantly with gemfibrozil (Part I) or rifampicin (Part II)

Other outcomes

  1. Incidence of treatment-emergent adverse events and serious adverse events

    Time frame: Up to 35 days (from first study drug administration to end of study visit)

    A treatment-emergent AE is any AE temporally associated with the use of a study treatment, whether or not considered related to the study treatment

  2. Incidence of safety events of interest

    Time frame: Up to 35 days (from first study drug administration to end of study visit)

    Include any abnormalities in ECG, vital signs or laboratory test results

Sponsors and collaborators

Lead sponsor

Actelion

Industry

Registry information

Official study title

A Single-center, Open-label, Randomized, Two-part, Two-treatment, Two-period Crossover Study to Investigate the Effect of Gemfibrozil or Rifampicin on the Pharmacokinetics of Selexipag and Its Metabolite ACT-333679 in Healthy Male Subjects.

Important dates

Study start
2016
Primary completion
2016
Study completion
2016
First posted
May 12, 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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