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Completed

NCT Number: NCT02791815

Potential Pharmacokinetic Interaction Between Selexipag and Midazolam in Healthy Male Subjects

The primary purpose of this study is to evaluate the effect of repeated doses of selexipag on the pharmacokinetics of a single oral dose of midazolam (i.e., how long and how much midazolam is present in the blood)

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Key information

Conditions

Healthy Subjects

Age range

18 year–45 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

Primary location

Investigator Site

Gières, 38610, France

About this study

In order to exclude an inductive effect of selexipag in the gastrointestinal tract, this study aims at investigating the effect of selexipag on the PK of midazolam, a sensitive substrate of both hepatic and intestinal cytochrome P450 3A4 (CYP3A4).

Who can participate

Healthy volunteers accepted: Yes

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

Key Inclusion Criteria:

  • Signed informed consent form
  • Age from 18 to 45 years (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:

  • Any contraindication to the study treatments
  • History or clinical evidence of any disease or medical / surgical 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 treatments
  • 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

Treatment and study plan

midazolam

Drug

Single oral dose of 7.5 mg midazolam (tablet)

Selexipag

Drug

Oral administration of selexipag (200 µg film-coated tablet) for 12 consecutive days (with a titration scheme from 400 to 1600 μg b.i.d. )

Other names: ACT-293987

Primary outcomes

  1. Cmax of midazolam following administration of midazolam alone and in combination with selexipag

    Time frame: From pre-dose up to 24 hours after midazolam admisnitration for each treatment period

    Cmax is the maximum observed plasma concentration and is directly derived from the individual plasma concentration time curves of midazolam

  2. AUC(0-inf) of midazolam following administration of midazolam alone and in combination with selexipag

    Time frame: From pre-dose up to 24 hours after midazolam admisnitration for each treatment period

    AUC(0-inf) is the area under the plasma concentration-time curves of midazolam, calculated from time 0 (pre-dose) to the extrapolated infinite time

Secondary outcomes

  1. Cmax of 1-hydroxymidazolam following administration of midazolam alone and in combination with selexipag

    Time frame: From pre-dose up to 24 hours after midazolam admisnitration

  2. AUC(0-inf) of 1-hydroxymidazolam following administration of midazolam alone and in combination with selexipag

    Time frame: From pre-dose up to 24 hours after midazolam admisnitration

  3. tmax of midazolam and 1-hydroxymidazolam following administration of midazolam alone and in combination with selexipag

    Time frame: From pre-dose up to 24 hours after midazolam admisnitration

    tmax is the time to reach Cmax of midazolam and its metabolite (1-hydroxymidazolam), respectively

  4. t½ of midazolam and 1-hydroxymidazolam following administration of midazolam alone and in combination with selexipag.

    Time frame: From pre-dose up to 24 hours after midazolam admisnitration

    t½ is the terminla half-life of midazolam and its metabolite (1-hydroxymidazolam), and corresponds to the period of time required for the concentration levels of midazolam and its metabolite to be reduced by one-half, respectively

  5. Trough concentration of selexipag and its metabolite ACT-333679 at steady-state

    Time frame: Days 1, 4, 7, 10,12 and 13

    Trough concentrations are measured before morning administration of selexipag

Other outcomes

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

    Time frame: Up to 39 days (from Day 1 of Period 1 to end of study of Period 2)

    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

Sponsors and collaborators

Lead sponsor

Actelion

Industry

Registry information

Official study title

A Single-center, Open-label, Randomized, Two-treatment Crossover Study to Investigate the Effect of Selexipag on the Pharmacokinetics of Midazolam and Its Metabolite 1-hydroxymidazolam in Healthy Male Subjects

Important dates

Study start
2016
Primary completion
2016
Study completion
2016
First posted
Jun 7, 2016
Registry last updated
Oct 13, 2016

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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