NCT02770222

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

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.

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 40 (actual)
• Sponsor: Actelion · Industry
• Sex: Male
• Age: 18 Years – 55 Years
• Healthy volunteers: Accepted

Summary

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).

Detailed description

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).

Conditions

• Healthy Subjects

Interventions

Type	Name	Description
DRUG	Selexipag	Two selexipag film-coated tablets of 200 µg as single oral dose (total dose = 400 µg)
DRUG	Gemfibrozil	Gemfibrozil film-coated tablet of 600 mg administered orally b.i.d. from Day 1 to Day 9
DRUG	Rifampicin	Rifampicin film-coated tablet of 600 mg administered orally o.d.from Day 1 to Day 9

Timeline

• Start date: 2016-06-01
• Primary completion: 2016-07-01
• Completion: 2016-07-01
• First posted: 2016-05-12
• Last updated: 2025-02-03