Selexipag, a selective prostacyclin receptor agonist in pulmonary arterial hypertension: a pharmacology review

Expert Review of Clinical Pharmacology
Jesús Honorato Pérez

Abstract

Pulmonary hypertension is defined by a mean pulmonary artery pressure ≥25 mm Hg at rest. Management of pulmonary arterial hypertension (PAH) includes specific drug therapy with calcium channel blockers in vasoreactive patients, or drugs approved for PAH in non-reactive patients that target the endothelin, nitric-oxide and prostacyclin pathways. Areas covered: The review covers receptor selectivity, pharmacokinetics, pharmacodynamics and adverse effects (AEs) of intravenous (IV) epoprostenol (synthetic prostacyclin); the prostacyclin analogs iloprost, beraprost, and treprostinil administered by IV, subcutaneous, inhaled or oral routes; and the oral selective prostacyclin receptor agonist selexipag. Expert commentary: Development of a selective prostacyclin receptor agonist has aimed at identifying compounds with improved pharmacological properties. The high selectivity of selexipag, and its active metabolite ACT-333679, for the prostacyclin receptor, in conjunction with pharmacokinetic properties that reduce peak-trough fluctuations and the up-titration regimen used at the start of treatment, are collectively considered to minimize AEs associated with prostacyclin use. In a large phase 3 study, selexipag-associated AEs were cons...Continue Reading

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Citations

Oct 11, 2019·Obstetrics and Gynecology·Stephanie R Martin, Alexandra Edwards
Feb 28, 2019·BioMed Research International·Andrea Sierra-SepúlvedaTatiana S Rodríguez-Reyna
Sep 12, 2020·Journal of Pharmacy Practice·Nathan J VerlindenRaymond L Benza
Jun 12, 2019·The Journal of Organic Chemistry·Siva Sankar Murthy BandaruAnant R Kapdi

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