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Purpose Targeting the prostacyclin pathway is an effective Key Points treatment option for pulmonary arterial hypertension (PAH). Patients with PAH have a deficiency of prostacyclin and Orally administered selexipag is in development for prostacyclin synthase. Selexipag is an orally available and the treatment of pulmonary arterial hypertension selective prostacyclin receptor (IP receptor) agonist. Selex- (PAH). Selexipag targets the prostacyclin pathway, ipag is hydrolyzed to its active metabolite ACT-333679, also one of the key pathways involved in the pathology of a selective and potent agonist at the IP receptor. PAH. Methods In this phase I study the pharmacokinetics (PK) In this phase I study, selexipag was well tolerated in and tolerability of single and multiple ascending doses of healthy male subjects receiving both single oral selexipag were investigated in a double-blind, placebo- doses up to 400 lg and multiple oral doses of twice- controlled manner in 64 healthy male subjects. An addi- daily 600 lg (following up-titration from 400 lg). tional group of 12 subjects received an open-label dose of selexipag 400 lg in the fasted condition and after a meal. Tolerability was improved when the drug was up- Results Maximum plasma concentrations of selexipag titrated in steps. and ACT-333679
American Journal of Cardiovascular Drugs – Springer Journals
Published: Apr 8, 2015
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