Endothelin-receptor antagonists in the management of pulmonary arterial hypertension: where do we stand?

References

• RubinLJMendozaJHoodMTreatment of primary pulmonary hypertension with continuous intravenous prostacyclin (epoprostenol): results of a randomized trialAnn Intern Med19901124854912107780
   PubMed Web of Science ®Google Scholar
• BarstRJRubinLJLongWAA comparison of continuous intravenous epoprostenol (prostacyclin) with conventional therapy for primary pulmonary hypertensionN Engl J Med19963342963018532025
   PubMed Web of Science ®Google Scholar
• BadeschDBTapsonVFMcGoonMDContinuous intravenous epoprostenol for pulmonary hypertension due to the scleroderma spectrum of disease: a randomized, controlled trialAnn Intern Med200013242543410733441
   PubMed Web of Science ®Google Scholar
• McLaughlinVVSitbonOBadeschDBSurvival with first-line bosentan in patients with primary pulmonary hypertensionEur Respir J20052524424915684287
   PubMed Web of Science ®Google Scholar
• ChenSJChenYFMengQCEndothelin-receptor antagonist bosentan prevents and reverses hypoxic pulmonary hypertension in ratsJ Appl Physiol199579212221318847282
   PubMed Web of Science ®Google Scholar
• HoeperMMTherapie der pulmonal arteriellen Hypertonie: Endothelin-Rezeptor-Antagonisten. [Treatment of pulmonary arterial hypertension: endothelin-receptor antagonists]Dtsch Med Wochenschr2006131S308S310 German17139593
   PubMedGoogle Scholar
• PestoSBegicZPrevljakSPecarEKukavicaNBegicEPulmonary hypertension: new trends of diagnostic and therapyMed Arch20167030330727703295
   PubMedGoogle Scholar
• VolkovAVIudkinaNNNikolaevaEVБозентан: существенное увеличение продолжительности жизни пациентов с легочной артериальной гипертонией, ассоциированной с системными ревматическими заболеваниями. Терапевтический архив. [Bosentan: a considerable increase in the survival of patients with pulmonary hypertension associated with systemic rheumatic diseases]Ter Arkh2014863239 Russian
   PubMed Web of Science ®Google Scholar
• MurdacaGLantieriFPuppoFBeneficial effects of long-term treatment with bosentan on the development of pulmonary arterial hypertension in patients with systemic sclerosisJ Int Med Res201644858927683147
   PubMed Web of Science ®Google Scholar
• PulidoTAdzerikhoIChannickRStudy with an endothelin receptor antagonist in pulmonary arterial hypertension to improve clinical outcome: macitentan and morbidity and mortality in pulmonary arterial hypertensionN Engl J Med201336980981823984728
   PubMed Web of Science ®Google Scholar
• GalieNBarberaJAFrostAEInitial use of ambrisentan plus tadalafil in pulmonary arterial hypertensionN Engl J Med201537383484426308684
   PubMed Web of Science ®Google Scholar
• IglarzMSteinerPWannerDReyMHessPClozelMVascular effects of endothelin receptor antagonists depends on their selectivity for ETA versus ETB receptors and on the functionality of endothelial ETB receptorsJ Cardiovasc Pharmacol20156633232725992919
   PubMed Web of Science ®Google Scholar
• CorrealeMTotaroALacedoniaDNovelty in treatment of pulmonary fibrosis: pulmonary hypertension drugs and othersCardiovasc Hematol Agents Med Chem20131116917824011020
   PubMedGoogle Scholar
• VatterHSeifertVAmbrisentan, a non-peptide endothelin receptor antagonistCardiovasc Drug Rev200624637616939634
   PubMed Web of Science ®Google Scholar
• BenzaRLMehtaSKeoghALawrenceECOudizRJBarstRJSitaxsentan treatment for patients with pulmonary arterial hypertension discontinuing bosentanJ Heart Lung Transplant200726636917234519
   PubMed Web of Science ®Google Scholar
• GalièNManesANegroLPalazziniMBacchi-ReggianiMLBranziAA meta-analysis of randomized controlled trials in pulmonary arterial hypertensionEur Heart J20093039440319155250
   PubMed Web of Science ®Google Scholar
• DonGWJosephFCelermajerDSCorteTJIronic case of hepatic dysfunction following the global withdrawal of sitaxentanIntern Med20124213511354
   Web of Science ®Google Scholar
• PatelTMcKeageKMacitentan: first global approvalDrugs20147412713324297706
   PubMed Web of Science ®Google Scholar
• BolliMHBossCBinkerThe discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N0-propyl-sulfamide (macitentan), an orally active, potent dual endothelin receptor antagonistJ Med Chem2012557849786122862294
   PubMed Web of Science ®Google Scholar
• DavenportAPHyndmanKADhaunNEndothelinPharmacol Rev20166835741826956245
   PubMed Web of Science ®Google Scholar
• SidhartaPNTreiberADingemanseJClinical pharmacokinetics and pharmacodynamics of the endothelin receptor antagonist macitentanClin Pharmacokinet20155445747125860376
   PubMed Web of Science ®Google Scholar
• GatfieldJGrandjeanCMSasseTSlow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial smooth muscle cellsPLoS One20127e4766223077657
   PubMed Web of Science ®Google Scholar
• IglarzMBossuAWannerDComparison of pharmacological activity of macitentan and bosentan in preclinical models of systemic and pulmonary hypertensionLife Sci201411833333924582812
   PubMed Web of Science ®Google Scholar
• RubinLJBadeschDBBarstRJBosentan therapy for pulmonary arterial hypertensionN Engl J Med200234689690311907289
   PubMed Web of Science ®Google Scholar
• DingemanseJSidhartaPNMaddreyWCEfficacy, safety and clinical pharmacology of macitentan in comparison to other endothelin receptor antagonists in the treatment of pulmonary arterial hypertensionExpert Opin Drug Saf20141339140524261583
   PubMed Web of Science ®Google Scholar
• D’AltoMAn update on the use of ambrisentan in pulmonary arterial hypertensionTher Adv Respir Dis2012633134322933513
   PubMed Web of Science ®Google Scholar
• Rivera-LebronBNRisbanoMGAmbrisentan: a review of its use in pulmonary arterial hypertensionTher Adv Respir Dis20171123324428425346
   PubMed Web of Science ®Google Scholar
• GalièNOlschewskiHOudizRJAmbrisentan for the treatment of pulmonary arterial hypertension: results of the ambrisentan in pulmonary arterial hypertension, randomized, double-blind, placebo-controlled, multicenter, efficacy (ARIES) study 1 and 2Circulation20081173010301918506008
   PubMed Web of Science ®Google Scholar
• OudizRJGalièNOlschewskiHLong-term ambrisentan therapy for the treatment of pulmonary arterial hypertensionJ Am Coll Cardiol2009541971198119909879
   PubMed Web of Science ®Google Scholar
• BadeschDBFeldmanJKeoghAARIES-3: ambrisentan therapy in a diverse population of patients with pulmonary hypertensionCardiovasc Ther201230939921884013
   PubMed Web of Science ®Google Scholar
• CoghlanJGGalièNBarberàJAInitial combination therapy with ambrisentan and tadalafil in connective tissue disease-associated pulmonary arterial hypertension (CTD-PAH): subgroup analysis from the AMBITION trialAnn Rheum Dis2017761219122728039187
   PubMed Web of Science ®Google Scholar
• GalièNHumbertMVachieryJL2015 ESC/ERS guidelines for the diagnosis and treatment of pulmonary hypertensionEur Heart J2016376711926320113
   PubMed Web of Science ®Google Scholar
• ShapiroSTorresFFeldmanJClinical and hemodynamic improvements after adding ambrisentan to background PDE5i therapy in patients with pulmonary arterial hypertension exhibiting a suboptimal therapeutic response (ATHENA-1)Respir Med2017126849228427554
   PubMed Web of Science ®Google Scholar
• Cartin-CebaRSwansonKIyerVWiesnerRHKrowkaMJSafety and efficacy of ambrisentan for the treatment of portopulmonary hypertensionChest201113910911420705798
   PubMed Web of Science ®Google Scholar
• FischerADentonCPMatucci-CerinicMAmbrisentan response in connective tissue disease-associated pulmonary arterial hypertension (CTD-PAH): a subgroup analysis of the ARIES-E clinical trialRespir Med201611725426327492539
   PubMed Web of Science ®Google Scholar
• HoeperMMMcLaughlinVVBarberáJAInitial combination therapy with ambrisentan and tadalafil and mortality in patients with pulmonary arterial hypertension: a secondary analysis of the results from the randomised, controlled AMBITION studyLancet Respir Med2016489490127745818
   PubMed Web of Science ®Google Scholar
• VachiéryJLHoeperMMPeacockAJAmbrisentan use for pulmonary arterial hypertension in a post-authorization drug registry: the Volibris tracking studyJ Heart Lung Transplant20173639940627282418
   PubMed Web of Science ®Google Scholar
• HassounPMZamanianRTDamicoRAmbrisentan and tadalafil up-front combination therapy in scleroderma-associated pulmonary arterial hypertensionAm J Respir Crit Care Med20151921102111026360334
   PubMed Web of Science ®Google Scholar
• D’AltoMRomeoEArgientoPInitial tadalafil and ambrisentan combination therapy in pulmonary arterial hypertension: clinical and haemodynamic long-term efficacy (ITALY study)J Cardiovasc Med (Hagerstown)201819121729215546
   PubMed Web of Science ®Google Scholar
• IglarzMBinkertCMorrisonKPharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonistJ Pharmacol Exp Ther200832773674518780830
   PubMed Web of Science ®Google Scholar
• SidhartaNvan GiersbergenPLDingemanseJSafety, tolerability, pharmacokinetics, and pharmacodynamics of macitentan, an endothelin receptor antagonist, in an ascending multiple dose study in healthy subjectsJ Clin Pharmacol2013531131113823900878
   PubMed Web of Science ®Google Scholar
• de KanterRSidhartaPNDelahayeSPhysiologically based pharmacokinetic modeling of macitentan: prediction of drug-drug interactionsClin Pharmacokinet20165536938026385839
   PubMed Web of Science ®Google Scholar
• Actelion PharmaceuticalsOpsumit (macitentan) tablets, for oral use [prescribing information]San Francisco, NCActelion2016
   Google Scholar
• European Medicines AgencyOpsumit (macitentan) [summary of product characteristics]LondonEMA2016
   Google Scholar
• BrudererSHopfgartnerGSeiberlingMAbsorption, distribution, metabolism, and excretion of macitentan, a dual endothelin receptor antagonist, in humansXenobiotica20124290191022458347
   PubMed Web of Science ®Google Scholar
• BrudererSMarjasonJSidhartaPNPharmacokinetics of macitentan in Caucasian and Japanese subjects: the influence of ethnicity and sexPharmacology20139133133823817130
   PubMed Web of Science ®Google Scholar
• AhnLYKimSEYiSPharmacokinetic–pharmacodynamic relationships of macitentan, a new endothelin receptor antagonist, after multiple dosing in healthy Korean subjectsAm J Cardiovasc Drugs20141437738524906252
   PubMed Web of Science ®Google Scholar
• SidhartaPNLindeggerNUlčIDingemanseJPharmacokinetics of the novel dual endothelin receptor antagonist macitentan in subjects with hepatic or renal impairmentJ Clin Pharmacol20145429130024122797
   PubMed Web of Science ®Google Scholar
• TreiberAAanismaaPde KanterRMacitentan does not interfere with hepatic bile salt transportJ Pharmacol Exp Ther201435013014324769543
   PubMed Web of Science ®Google Scholar
• BrudererSAanismaaPHomeryMCEffect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue-targeting dual endothelin receptor antagonistAAPS J201214687822189899
   PubMed Web of Science ®Google Scholar
• AtsmonJDingemanseJShaikevichDInvestigation of the effects of ketoconazole on the pharmacokinetics of macitentan, a novel dual endothelin receptor antagonist, in healthy subjectsClin Pharmacokinet20135268569223568224
   PubMed Web of Science ®Google Scholar
• HurstNPellekMDingemanseJLack of pharmacokinetic interactions between macitentan and a combined oral contraceptive in healthy female subjectsJ Clin Pharmacol20165666967426381054
   PubMed Web of Science ®Google Scholar
• SidhartaPNDietrichHDingemanseJInvestigation of the effect of macitentan on the pharmacokinetics and pharmacodynamics of warfarin in healthy male subjectsClin Drug Investig201434545552
   PubMed Web of Science ®Google Scholar
• SidhartaPNvan GiersbergenPLWolztMDingemanseJInvestigation of mutual pharmacokinetic interactions between macitentan, a novel endothelin receptor antagonist, and sildenafil in healthy subjectsBr J Clin Pharmacol2014781035104224962473
   PubMed Web of Science ®Google Scholar
• ZisowskyJSidhartaPNKrauseADingemanseJPharmacokinetic/pharmacodynamic analyses in SERAPHIN, a randomized, controlled study of macitentan in patients with pulmonary arterial hypertensionClin Pharmacol Drug Dev2013229
   Google Scholar
• KimNHChinKMMuros-le RouzicEOpsumit Users Registry (OPUS): insights into the safety and tolerability of OpsumitAm J Respir Crit Care Med2016193A7396
   Web of Science ®Google Scholar
• BlokIMvan RielACvan DijkAPMulderBJBoumaBJFrom bosentan to macitentan for pulmonary arterial hypertension and adult congenital heart disease: further improvement?Int J Cardiol2017227515227846462
   PubMed Web of Science ®Google Scholar
• SafdarZThakurAFrostATolerability of switch to macitentan from bosentan in pulmonary arterial hypertensionSouth Med J201711022322828257550
   PubMed Web of Science ®Google Scholar
• OlschewskiHSimonneauGGalièNInhaled iloprost for severe pulmonary hypertensionN Engl J Med200234732232912151469
   PubMed Web of Science ®Google Scholar
• RubinLJBadeschDBBarstRJBosentan therapy for pulmonary arterial hypertensionN Engl J Med200234689690311907289
   PubMed Web of Science ®Google Scholar
• SimonneauGBarstRJGalièNContinuous subcutaneous infusion of treprostinil, a prostacyclin analog, in patients with pulmonary arterial hypertension: a double-blind, randomized, placebo-controlled trialAm J Respir Crit Care Med200216580080411897647
   PubMed Web of Science ®Google Scholar
• GalièNGhofraniHATorbickiASildenafil citrate therapy for pulmonary arterial hypertensionN Engl J Med20053532148215716291984
   PubMed Web of Science ®Google Scholar
• GalièNBrundageBGhofraniHATadalafil therapy for pulmonary arterial hypertensionCirculation20091192894290319470885
   PubMed Web of Science ®Google Scholar
• GhofraniHASimonneauGD’ArminiAMMacitentan for the treatment of inoperable chronic thromboembolic pulmonary hypertension (MERIT-1): results from the multicentre, phase 2, randomised, double-blind, placebo-controlled studyLancet Respir Med201710785794
   Google Scholar
• GalièNJansaPPulidoTSERAPHIN haemodynamic sub-study: the effect of the dual endothelin receptor antagonist macitentan on haemodynamic parameters and NT-proBNP levels and their association with disease progression in patients with pulmonary arterial hypertensionEur Heart J2017381147115528329315
   PubMed Web of Science ®Google Scholar
• ChannickRNDelcroixMGhofraniHAEffect of macitentan on hospitalizations: results from the SERAPHIN trialJACC Heart Fail201531825457902
   PubMed Web of Science ®Google Scholar
• SimonneauGChannickRNDelcroixMIncident and prevalent cohorts with pulmonary arterial hypertension: insight from SERAPHINEur Respir J2015461711172026493786
   PubMed Web of Science ®Google Scholar
• ChannickRNDelcroixMGalieNThe effect of macitentan on long-term outcomes in patients with pulmonary arterial hypertension by WHO functional class: data from the randomized controlled SERAPHIN studyAm J Respir Crit Care Med2014189A4783
   Web of Science ®Google Scholar
• SitbonOChannickRNDelcroixMMacitentan reduces the risk of morbidity and mortality irrespective of the presence or absence of right ventricular (RV) impairment: results from the randomised SERAPHIN trial in pulmonary arterial hypertension (PAH)Eur Respir J2014443419
   Web of Science ®Google Scholar
• MehtaSSastryBSouzaRMacitentan improves health-related quality of life for patients with pulmonary arterial hypertension: results from the randomized controlled SERAPHIN trialChest201715110611827671974
   PubMed Web of Science ®Google Scholar
• HerbertSGin-SingWHowardLTullohRMEarly experience of macitentan for pulmonary arterial hypertension in adult congenital heart diseaseHeart Lung Circ2017261113111628237536
   PubMed Web of Science ®Google Scholar
• PizarroCMeyer-ArendJMSchuelerRImpact of macitentan on right ventricular myocardial function in pulmonary arterial hypertensionInt J Cardiol201621443844127096961
   PubMed Web of Science ®Google Scholar
• Duo-JiMMLongZWComparative efficacy and acceptability of endothelin receptor antagonists for pulmonary arterial hypertension: a network meta-analysisInt J Cardiol2017234909828233631
   PubMed Web of Science ®Google Scholar
• WeiAGuZLiJClinical adverse effects of endothelin receptor antagonists: insights from the meta-analysis of 4894 patients from 24 randomized double-blind placebo-controlled clinical trialsJ Am Heart Assoc20165e00389627912207
   PubMed Web of Science ®Google Scholar
• ZhengYGMaHHuECLiuGChenGXiongCMOral targeted therapies in the treatment of pulmonary arterial hypertension: a meta-analysis of clinical trialsPulm Pharmacol Ther20142924124925173912
   PubMed Web of Science ®Google Scholar
• DrozdKAhmadiADengYEffects of an endothelin receptor antagonist, macitentan, on right ventricular substrate utilization and function in a Sugen 5416/hypoxia rat model of severe pulmonary arterial hypertensionJ Nucl Cardiol2016619791989
   Google Scholar
• NielsenEASunMHonjoOHjortdalVERedingtonANFriedbergMKDual endothelin receptor blockade abrogates right ventricular remodeling and biventricular fibrosis in isolated elevated right ventricular afterloadPLoS One201611e014676726765263
   PubMed Web of Science ®Google Scholar
• LiuXKhadtareNPatelHStephaniRCantorJTime-dependent effects of HJP272, an endothelin receptor antagonist, in bleomycin-induced pulmonary fibrosisPulm Pharmacol Ther20174516416928619646
   PubMed Web of Science ®Google Scholar
• EgidoJRojas-RiveraJMasSAtrasentan for the treatment of diabetic nephropathyExpert Opin Investig Drugs201726741750
   PubMed Web of Science ®Google Scholar
• ActelionEffects of the combination of bosentan and sildenafil versus sildenafil monotherapy on pulmonary arterial hypertension (PAH) (COMPASS-2) Available from: https://clinicaltrials.gov/ct2/show/NCT00303459. NLM identifier: NCT00303459Accessed April 5, 2018
   Google Scholar