Selexipag in the treatment of pulmonary arterial hypertension: design, development, and therapy

References

• ClappLHFinneyPTurcatoSTranSRubinLJTinkerADifferential effects of stable prostacyclin analogs on smooth muscle proliferation and cyclic AMP generation in human pulmonary arteryAm J Respir Cell Mol Biol200226219420111804870
   PubMed Web of Science ®Google Scholar
• HumbertMMorrellNWArcherSLCellular and molecular pathobiology of pulmonary arterial hypertensionJ Am Coll Cardiol20044312 Suppl S13s24s15194174
   PubMed Web of Science ®Google Scholar
• OidaHNambaTSugimotoYIn situ hybridization studies of prostacyclin receptor mRNA expression in various mouse organsBr J Pharmacol19951167282828378680713
   PubMed Web of Science ®Google Scholar
• RubinLJGrovesBMReevesJTFrosolonoMHandelFCatoAEProstacyclin-induced acute pulmonary vasodilation in primary pulmonary hypertensionCirculation19826623343387046988
   PubMed Web of Science ®Google Scholar
• HoshikawaYVoelkelNFGesellTLProstacyclin receptor-dependent modulation of pulmonary vascular remodelingAm J Respir Crit Care Med2001164231431811463607
   PubMed Web of Science ®Google Scholar
• NagayaNYokoyamaCKyotaniSGene transfer of human prostacyclin synthase ameliorates monocrotaline-induced pulmonary hypertension in ratsCirculation2000102162005201011034952
   PubMed Web of Science ®Google Scholar
• ChristmanBWMcPhersonCDNewmanJHAn imbalance between the excretion of thromboxane and prostacyclin metabolites in pulmonary hypertensionN Engl J Med1992327270751603138
   PubMed Web of Science ®Google Scholar
• TuderRMCoolCDGeraciMWProstacyclin synthase expression is decreased in lungs from patients with severe pulmonary hypertensionAm J Respir Crit Care Med199915961925193210351941
   PubMed Web of Science ®Google Scholar
• FalcettiEHallSMPhillipsPGSmooth muscle proliferation and role of the prostacyclin (IP) receptor in idiopathic pulmonary arterial hypertensionAm J Respir Crit Care Med201018291161117020622039
   PubMed Web of Science ®Google Scholar
• StearmanRSCorneliusARLuXFunctional prostacyclin synthase promoter polymorphisms. Impact in pulmonary arterial hypertensionAm J Respir Crit Care Med201418991110112024605778
   PubMed Web of Science ®Google Scholar
• BarstRJRubinLJLongWAA comparison of continuous intravenous epoprostenol (prostacyclin) with conventional therapy for primary pulmonary hypertensionN Engl J Med199633452963018532025
   PubMed Web of Science ®Google Scholar
• GalieNHumbertMVachieryJLEffects of beraprost sodium, an oral prostacyclin analogue, in patients with pulmonary arterial hypertension: a randomized, double-blind, placebo-controlled trialJ Am Coll Cardiol20023991496150211985913
   PubMed Web of Science ®Google Scholar
• BarstRJMcGoonMMcLaughlinVBeraprost therapy for pulmonary arterial hypertensionJ Am Coll Cardiol200341122119212512821234
   PubMed Web of Science ®Google Scholar
• DemolisJLRobertAMourenMFunck-BrentanoCJaillonPPharmacokinetics and platelet antiaggregating effects of beraprost, an oral stable prostacyclin analogue, in healthy volunteersJ Cardiovasc Pharmacol19932257117167506323
   PubMed Web of Science ®Google Scholar
• TapsonVFTorresFKermeenFOral treprostinil for the treatment of pulmonary arterial hypertension in patients on background endothelin receptor antagonist and/or phosphodiesterase type 5 inhibitor therapy (the FREEDOM-C study): a randomized controlled trialChest201214261383139022628490
   PubMed Web of Science ®Google Scholar
• TapsonVFJingZCXuKFOral treprostinil for the treatment of pulmonary arterial hypertension in patients receiving background endothelin receptor antagonist and phosphodiesterase type 5 inhibitor therapy (the FREEDOM-C2 study): a randomized controlled trialChest2013144395295823669822
   PubMed Web of Science ®Google Scholar
• JingZCParikhKPulidoTEfficacy and safety of oral treprostinil monotherapy for the treatment of pulmonary arterial hypertension: a randomized, controlled trialCirculation2013127562463323307827
   PubMed Web of Science ®Google Scholar
• WhiteRJAllenRTorresFSustained plasma concentrations of treprostinil following chronic dosing of oral treprostinil in patients with pulmonary arterial hypertensionAm J Respir Crit Care Med2009179A3360
   Web of Science ®Google Scholar
• WadeMBakerFJRoscignoRDellaMaestraWHuntTLLaiAAAbsolute bioavailability and pharmacokinetics of treprostinil sodium administered by acute subcutaneous infusionJ Clin Pharmacol2004441838814681345
   PubMed Web of Science ®Google Scholar
• Orinetram (Oral Treprostinil) Prescribing Information Available from: https://www.orenitram.com/pdf/Orenitram_Full_Prescribing_Information.pdfAccessed July 12, 2016
   Google Scholar
• Beraprost 314d trial (BEAT) Available from: https://clinicaltrials.gov/ct2/show/NCT01908699Accessed July 26, 2016
   Google Scholar
• Freedom Ev Trial (Oral Treprostinil) Available from: https://clinicaltrials.gov/ct2/show/NCT01560624Accessed July 29, 2016
   Google Scholar
• KaufmannPOkuboKBrudererSPharmacokinetics and toler-ability of the novel oral prostacyclin IP receptor agonist selexipagAm J Cardiovasc Drugs201515319520325850750
   PubMed Web of Science ®Google Scholar
• U.S Department of Health and Human Services, Food and Drug AdministrationUS Prescribing Information: Uptravi (Selexipag) Tables, for Oral Use20152016 Available from: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207947s000lbl.pdfAccessed September 25, 2016
   Google Scholar
• KuwanoKHashinoANodaKKosugiKKuwabaraKA long-acting and highly selective prostacyclin receptor agonist prodrug, 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl) acetam ide (NS-304), ameliorates rat pulmonary hypertension with unique relaxant responses of its active form, {4-[(5,6-diphenylpyrazin-2-yl) (isopropyl)amino]butoxy}acetic acid (MRE-269), on rat pulmonary arteryJ Pharmacol Exp Ther2008326369169918552131
   PubMed Web of Science ®Google Scholar
• MorrisonKStuderRErnstRHaagFKauserKClozelMDifferential effects of selexipag [corrected] and prostacyclin analogs in rat pulmonary arteryJ Pharmacol Exp Ther2012343354755522918043
   PubMed Web of Science ®Google Scholar
• OkaMFaganKAJonesPLMcMurtryIFTherapeutic potential of RhoA/Rho kinase inhibitors in pulmonary hypertensionBr J Pharmacol2008155444445418536743
   PubMed Web of Science ®Google Scholar
• SimonneauGTorbickiAHoeperMMSelexipag: an oral, selective prostacyclin receptor agonist for the treatment of pulmonary arterial hypertensionEur Respir J201240487488022362844
   PubMed Web of Science ®Google Scholar
• SitbonOChannickRChinKMSelexipag for the treatment of pulmonary arterial hypertensionN Engl J Med2015373262522253326699168
   PubMed Web of Science ®Google Scholar
• BarstRJOudizRJBeardsworthATadalafil monotherapy and as add-on to background bosentan in patients with pulmonary arterial hypertensionJ Heart Lung Transplant201130663264321256048
   PubMed Web of Science ®Google Scholar
• GalieNHumbertMVachieryJLESC/ERS guidelines for the diagnosis and treatment of pulmonary hypertension: the joint task force for the diagnosis and treatment of pulmonary hypertension of the European Society of Cardiology (ESC) and the European Respiratory Society (ERS): endorsed by: Association for European Paediatric and Congenital Cardiology (AEPC), International Society for Heart and Lung Transplantation (ISHLT)Eur Respir J201546490397526318161
   PubMed Web of Science ®Google Scholar
• BrudererSHurstNKaufmannPDingemanseJMultiple-dose up-titration study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of selexipag, an orally available selective prostacyclin receptor agonist, in healthy subjectsPharmacology2014943–414815625277144
   PubMed Web of Science ®Google Scholar
• MubarakKKA review of prostaglandin analogs in the management of patients with pulmonary arterial hypertensionRespir Med2010104192119683911
   PubMed Web of Science ®Google Scholar
• KaufmannPCruzHGKrauseAUlcIHalabiADingemanseJPharmacokinetics of the novel oral prostacyclin receptor agonist selexipag in subjects with hepatic or renal impairmentBr J Clin Pharmacol201682236937927062188
   PubMed Web of Science ®Google Scholar
• ClappLHGurungRThe mechanistic basis of prostacyclin and its stable analogues in pulmonary arterial hypertension: role of membrane versus nuclear receptorsProstaglandins Other Lipid Mediat2015120567125917921
   PubMed Web of Science ®Google Scholar
• AsakiTKuwanoKMorrisonKGatfieldJHamamotoTClozelMSelexipag: an oral and selective IP prostacyclin receptor agonist for the treatment of pulmonary arterial hypertensionJ Med Chem201558187128713726291199
   PubMed Web of Science ®Google Scholar
• LuAZuoCHeYEP3 receptor deficiency attenuates pulmonary hypertension through suppression of Rho/TGF-beta1 signalingJ Clin Invest201512531228124225664856
   PubMed Web of Science ®Google Scholar
• QianYMJonesRLChanKMStockAIHoJKPotent contractile actions of prostanoid EP3-receptor agonists on human isolated pulmonary arteryBr J Pharmacol199411323693747834185
   PubMed Web of Science ®Google Scholar
• WalchLde MontprevilleVBrinkCNorelXProstanoid EP(1)- and TP-receptors involved in the contraction of human pulmonary veinsBr J Pharmacol200113481671167811739243
   PubMed Web of Science ®Google Scholar
• WhittleBJSilversteinAMMottolaDMClappLHBinding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonistBiochem Pharmacol2012841687522480736
   PubMed Web of Science ®Google Scholar
• MorrisonKErnstRHessPStuderRClozelMSelexipag: a selective prostacyclin receptor agonist that does not affect rat gastric functionJ Pharmacol Exp Ther2010335124925520660124
   PubMed Web of Science ®Google Scholar
• BenyahiaCBoukaisKGomezIA comparative study of PGI2 mimetics used clinically on the vasorelaxation of human pulmonary arteries and veins, role of the DP-receptorProstaglandins Other Lipid Mediat2013107485523850788
   PubMed Web of Science ®Google Scholar
• KnebelSMSpragueRSStephensonAHProstacyclin receptor expression on platelets of humans with type 2 diabetes is inversely correlated with hemoglobin A1c levelsProstaglandins Other Lipid Mediat2015116–117131135
   PubMed Web of Science ®Google Scholar
• SmythEMAustinSCReillyMPFitzGeraldGAInternalization and sequestration of the human prostacyclin receptorJ Biol Chem200027541320373204510889200
   PubMed Web of Science ®Google Scholar
• KuwanoKHashinoAAsakiT2-[4-[(5,6-diphenylpyrazin-2-yl) (isopropyl)amino]butoxy]-N-(methylsulfonyl)acetam ide (NS-304), an orally available and long-acting prostacyclin receptor agonist prodrugJ Pharmacol Exp Ther200732231181118817545310
   PubMed Web of Science ®Google Scholar
• MorrisonKWannerDGatfieldJGnerreCHessPClozelMRepeated oral administration of the selective prostacyclin receptor agonist selexipag does not cause tachyphylaxis in spontaneously hypertensive rats [Abstract]J Am Coll Cardiol20156510SA1558
   Google Scholar
• GatfieldJMenyhartKMorrisonKNaylerOThe non-prostanoid prostacyclin receptor agonist ACT-333679, the active metabolite of selexipag, is characterized by low beta-arrestin recruitment and receptor internalization activity [abstract]J Am Coll Cardiol20156510SA1542
   Google Scholar
• McLaughlinVVGenthnerDEPanellaMMRichSReduction in pulmonary vascular resistance with long-term epoprostenol (prostacyclin) therapy in primary pulmonary hypertensionN Engl J Med199833852732779445406
   PubMed Web of Science ®Google Scholar
• GalieNBarberaJAFrostAEInitial use of ambrisentan plus tadalafil in pulmonary arterial hypertensionN Engl J Med2015373983484426308684
   PubMed Web of Science ®Google Scholar
• GalieNCorrisPAFrostAUpdated treatment algorithm of pulmonary arterial hypertensionJ Am Coll Cardiol20136225 SupplD60D7224355643
   PubMed Web of Science ®Google Scholar
• SitbonOJaisXSavaleLUpfront triple combination therapy in pulmonary arterial hypertension: a pilot studyEur Respir J20144361691169724627535
   PubMed Web of Science ®Google Scholar