Trial reportAmerican journal of cardiovascular drugs : drugs, devices, and other interventions2015
Pharmacokinetics and Tolerability of the Novel Oral Prostacyclin IP Receptor Agonist Selexipag.
Trial report in American journal of cardiovascular drugs : drugs, devices, and other interventions, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
27 citing papers in PubMed.
- Temporarily switching from oral to intravenous selexipag in patients with pulmonary arterial hypertension: safety, tolerability, and pharmacokinetic results from an open-label, phase III study.Respiratory research · 2021Trial
- Biocomparison Study of Adult and Paediatric Dose Strengths of the Prostacyclin Receptor Agonist Selexipag.European journal of drug metabolism and pharmacokinetics · 2018Trial
- Effect of gemfibrozil and rifampicin on the pharmacokinetics of selexipag and its active metabolite in healthy subjects.British journal of clinical pharmacology · 2017Trial
- A pharmacokinetic drug-drug interaction study between selexipag and midazolam, a CYP3A4 substrate, in healthy male subjects.European journal of clinical pharmacology · 2017Trial
- Absolute oral bioavailability of selexipag, a novel oral prostacyclin IP receptor agonist.European journal of clinical pharmacology · 2017Trial
- Structure-optimization and structure-activity relationship of diphenylpyrazinyl aminoalkoxyacetic acid derivatives: piperidine substitution and hydrophobic modification as key strategies for IP receptor agonists.Journal of computer-aided molecular design · 2026Article
- Experience with selexipag in triple therapy for pulmonary arterial hypertension in Chinese children.BMC pediatrics · 2026Article
- Evaluation and Management of Sepsis in Pulmonary Hypertension.Journal of intensive care medicine · 2025Review
- The Role of Intravenous Selexipag in Managing PAH and Bridging Gaps in Oral Treatment: A Narrative Review.Therapeutics and clinical risk management · 2025Review
- Antiproliferative effect of selexipag active metabolite MRE-269 on pulmonary arterial smooth muscle cells from patients with chronic thromboembolic pulmonary hypertension.Pulmonary circulation · 2023Article
- Effect of quercetin on the pharmacokinetics of selexipag and its active metabolite in beagles.Pharmaceutical biology · 2022Article
- Article
- Management of Pulmonary Arterial Hypertension.Current cardiovascular risk reports · 2021Review
- The selective PGI2 receptor agonist selexipag ameliorates Sugen 5416/hypoxia-induced pulmonary arterial hypertension in rats.PloS one · 2020Article
- Predictive Value of Microdose Pharmacokinetics.Clinical pharmacokinetics · 2019Review
- Treatment of pulmonary arterial hypertension: A review of drugs available for advanced therapy.African journal of thoracic and critical care medicine · 2019Review
- Selexipag in the management of pulmonary arterial hypertension: an update.Drug, healthcare and patient safety · 2019Article
- Pharmacokinetics of the novel oral prostacyclin receptor agonist selexipag in subjects with hepatic or renal impairment.British journal of clinical pharmacology · 2016Article
- Selexipag: First Global Approval.Drugs · 2016Review
- Selexipag in the treatment of pulmonary arterial hypertension: design, development, and therapy.Drug design, development and therapy · 2016Review
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Authors and funding
7 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTargeting the prostacyclin pathway is an effective treatment option for pulmonary arterial hypertension (PAH). Patients with PAH have a deficiency of prostacyclin and prostacyclin synthase. Selexipag is an orally available and selective prostacyclin receptor (IP receptor) agonist. Selexipag is hydrolyzed to its active metabolite ACT-333679, also a selective and potent agonist at the IP receptor.
methodsIn this phase I study the pharmacokinetics (PK) and tolerability of single and multiple ascending doses of selexipag were investigated in a double-blind, placebo-controlled manner in 64 healthy male subjects. An additional group of 12 subjects received an open-label dose of selexipag 400 μg in the fasted condition and after a meal.
resultsMaximum plasma concentrations of selexipag and ACT-333679 were reached within 2.5 and 4 h, respectively, with mean half-lives of 0.7-2.3 and 9.4-14.22 h. In the presence of food, exposure to ACT-333679 was decreased by 27 %. The most frequent adverse event was headache. Selexipag was well tolerated up to a single dose of 400 μg and multiple doses of 600 μg following an up-titration step. No relevant treatment-related effects on vital signs, clinical laboratory, and electrocardiogram (ECG) parameters were detected.
conclusionSelexipag exhibits a good tolerability profile and PK properties that warrant further investigation.
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