Absolute oral bioavailability of selexipag, a novel oral prostacyclin IP receptor agonist

Kaufmann, Priska; Hurst, Noémie; Astruc, B; Dingemanse, Jasper

doi:10.1007/s00228-016-2164-4

Cited by 20 publications

(21 citation statements)

References 15 publications

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“…The structures of both compounds have been published previously . An absolute bioavailability study in healthy subjects showed that the clearance of selexipag is 17.9 l h –1 , the volume of distribution 11.7 l and the absolute bioavailability 49.4% . Following single‐ and multiple‐dose oral administration of selexipag to healthy subjects, the pharmacokinetics (PK) of selexipag and ACT‐333679 were dose proportional .…”

Section: Introductionmentioning

confidence: 99%

Effect of gemfibrozil and rifampicin on the pharmacokinetics of selexipag and its active metabolite in healthy subjects

Bruderer

Petersen-Sylla

Boehler

et al. 2017

Brit J Clinical Pharma

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Section: Introductionmentioning

confidence: 99%

Effect of gemfibrozil and rifampicin on the pharmacokinetics of selexipag and its active metabolite in healthy subjects

Bruderer

Petersen-Sylla

Boehler

et al. 2017

Brit J Clinical Pharma

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“…Bioavailability of selexipag after oral administration was demonstrated to be approximately 50%. 5,6,9–16…”

Section: Discussionmentioning

confidence: 99%

Hemodynamic and clinical effects of selexipag in children with pulmonary hypertension

et al. 2020

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Selexipag is an oral prostacyclin receptor agonist; it was recently approved for use in adults with pulmonary arterial hypertension. The safety and efficacy of selexipag has not yet been determined in the pediatric population. We describe short-term hemodynamic and clinical data with selexipag therapy in four pediatric patients with pulmonary hypertension. We reviewed clinical, echocardiographic, and hemodynamic data. One patient was transitioned from subcutaneous treprostinil to selexipag, and in three patients, selexipag was added as a third agent. Drug dosing was attained empirically based on patient body size. A follow-up catheterization was performed 12–18 months after initiation of selexipag therapy. All four patients tolerated selexipag well, without significant side effects. One patient transitioned successfully from subcutaneous treprostinil to selexipag. None of the four patients had clinical deterioration. In three patients who were able to perform a 6-minute walk test, pre and post selexipag distances were 350 and 400, 409 and 390, and 300 and 360 m, respectively. Echocardiograms showed no significant changes. Catheterization showed a variable change in pulmonary vascular resistance (small decrease in three patients and increase in one patient). Brain natriuretic peptide levels before and after selexipag in the four patients were 38 and 49, 33 and 54, 29 and 25, and 12 and 14 pg/mL, respectively. Selexipag use for 16–28 months was safe in four pediatric patients; none of them had clinical deterioration. Larger number of patients and longer follow-up intervals are necessary before further recommendations can be made.

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“…PGI 2 analogs have been used clinically for treatment of several diseases characterized by ischemia (37). Recently, orally active prostacyclin agonist has been used in patients with pulmonary hypertension (38). Consequently, PGI 2 analogs and agonists are promising molecules for enhancing the effects of angiogenesis-based treatments and may be applicable for tooth revascularization and regeneration.…”

Section: Discussionmentioning

confidence: 99%

Prolonged release of iloprost enhances pulpal blood flow and dentin bridge formation in a rat model of mechanical tooth pulp exposure

et al. 2019

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The aim of this study was to investigate the effect of prolonged release of iloprost, a prostacyclin analog, on angiogenesis and dental pulp healing in a rat model of mechanical pulp exposure. The profile of iloprost release from poly (lactic-co-glycolic) acid (PLGA) microspheres was evaluated, and expression of vascular endothelial growth factor (VEGF) mRNA was determined. The molars of rats were subjected to mechanical pulp exposure and 5 different forms of treatment: Ca(OH) 2 , PLGA (blank), iloprost, and iloprost/PLGA. Blood flow was determined at 0, 3, and 7 days using laser Doppler flowmetry. After 30 days, the tooth specimens were collected, and subjected to micro-CT and immunohistological analysis. The results showed that iloprost release from the microspheres was prolonged for 4 days, and that the treatment increased tooth blood flow for up to 7 days. At 30 days, an increase of mineralized tissue formation and dentin bridge formation was observed in the iloprost and iloprost/PLGA microsphere groups. VEGF expression was significantly increased in the iloprost/PLGA microsphere group relative to the other groups. In conclusion, this PLGA microsphere iloprost delivery system significantly increased dental pulp blood flow in a prolonged manner and increased tertiary dentin formation in this rat pulp injury model. Prolonged prostacyclin release could be a potentially useful approach for regeneration of dental pulp.

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Absolute oral bioavailability of selexipag, a novel oral prostacyclin IP receptor agonist

Abstract: A single i.v. administration of selexipag in healthy subjects was safe and well-tolerated. The bioavailability of selexipag after oral administration is approximately 50%.

Cited by 20 publications

References 15 publications

Effect of gemfibrozil and rifampicin on the pharmacokinetics of selexipag and its active metabolite in healthy subjects

Effect of gemfibrozil and rifampicin on the pharmacokinetics of selexipag and its active metabolite in healthy subjects

Hemodynamic and clinical effects of selexipag in children with pulmonary hypertension

Prolonged release of iloprost enhances pulpal blood flow and dentin bridge formation in a rat model of mechanical tooth pulp exposure

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