Single- and multiple-dose tolerability, safety, pharmacokinetics, and pharmacodynamics of the dual endothelin receptor antagonist aprocitentan in healthy adult and elderly subjects

References

• MillsKTBundyJDKellyTNGlobal disparities of hypertension prevalence and control: a systematic analysis of population-based studies from 90 countriesCirculation2016134644145027502908
   PubMed Web of Science ®Google Scholar
• MoserMSetaroJFClinical practice. Resistant or difficult-to-control hypertensionN Engl J Med2006355438539216870917
   PubMed Web of Science ®Google Scholar
• ManciaGFagardRNarkiewiczKTask Force Members2013 ESH/ESC guidelines for the management of arterial hypertension: the task force for the management of arterial hypertension of the European Society of hypertension (ESH) and of the European Society of Cardiology (ESC)J Hypertens20133171281135723817082
   PubMed Web of Science ®Google Scholar
• MakaniHBangaloreSDesouzaKAShahAMesserliFHEfficacy and safety of dual blockade of the renin–angiotensin system: meta-analysis of randomised trialsBMJ2013346f36023358488
   PubMed Web of Science ®Google Scholar
• YusufSTeoKKPogueJTelmisartan, ramipril, or both in patients at high risk for vascular eventsN Engl J Med2008358151547155918378520
   PubMed Web of Science ®Google Scholar
• JuurlinkDNMamdaniMMLeeDSRates of hyperkalemia after publication of the Randomized Aldactone Evaluation studyN Engl J Med2004351654355115295047
   PubMed Web of Science ®Google Scholar
• HorowitzBMiskulinDZagerPEpidemiology of hypertension in CKDAdv Chronic Kidney Dis2015222889525704344
   PubMed Web of Science ®Google Scholar
• Gijón-CondeTGracianiABanegasJRResistant hypertension: demography and clinical characteristics in 6,292 patients in a primary health care settingRev Esp Cardiol (Engl Ed)201467427027624774589
   PubMed Web of Science ®Google Scholar
• FoodUSAdministrationDrugHypertension: Conducting Studies of Drugs to Treat Patients on a Background of Multiple Antihypertensive Drugs Guidance for IndustrySilver Spring, MDUS Food and Drug Administration2018
   Google Scholar
• DonatelliMCollettiIBucaloMLRussoVVergaSPlasma endothelin levels in NIDDM patients with macroangiopathyDiabetes Res19942541591647648786
   PubMedGoogle Scholar
• CardilloCKilcoyneCMWaclawiwMCannonROPanzaJARole of endothelin in the increased vascular tone of patients with essential hypertensionHypertension199933275375810024340
   PubMed Web of Science ®Google Scholar
• DavenportAPHyndmanKADhaunNEndothelinPharmacol Rev201668235741826956245
   PubMed Web of Science ®Google Scholar
• YanagisawaMKuriharaHKimuraSA novel potent vasoconstrictor peptide produced by vascular endothelial cellsNature198833261634114152451132
   PubMed Web of Science ®Google Scholar
• DavenportAPO’ReillyGKucREEndothelin ETA and ETB mRNA and receptors expressed by smooth muscle in the human vasculature: majority of the ETA sub-typeBr J Pharmacol19951146111011167620699
   PubMed Web of Science ®Google Scholar
• ZhangMLuoBChenSJAbramsGAFallonMBEndothelin-1 stimulation of endothelial nitric oxide synthase in the pathogenesis of hepatopulmonary syndromeAm J Physiol19992775G944G95210564099
   PubMedGoogle Scholar
• WinklesJAAlbertsGFBrogiELibbyPEndothelin-1 and endothelin receptor mRNA expression in normal and atherosclerotic human arteriesBiochem Biophys Res Commun19931912108110888466485
   PubMed Web of Science ®Google Scholar
• DupuisJGoreskyCAFournierAPulmonary clearance of circulating endothelin-1 in dogs in vivo: exclusive role of ETB receptorsJ Appl Physiol (1985)1996814151015158904561
   PubMed Web of Science ®Google Scholar
• DupuisJStewartDJCernacekPGosselinGHuman pulmonary circulation is an important site for both clearance and production of endothelin-1Circulation1996947157815848840847
   PubMed Web of Science ®Google Scholar
• GeYBagnallAStricklettPKCollecting duct-specific knockout of the endothelin B receptor causes hypertension and sodium retentionAm J Physiol Renal Physiol20062916F1274F128016868309
   PubMed Web of Science ®Google Scholar
• GaddamKKNishizakaMKPratt-UbunamaMNCharacterization of resistant hypertension: association between resistant hypertension, aldosterone, and persistent intravascular volume expansionArch Intern Med2008168111159116418541823
   PubMedGoogle Scholar
• TrenszFBortolamiolCKrambergMPharmacological characterization of APROCITENTAN, a dual endothelin receptor antagonist, alone and in combination with blockers of the renin angiotensin system, in two models of experimental hypertensionJ Pharmacol Exp Ther2019368346247330622171
   PubMed Web of Science ®Google Scholar
• PulidoTAdzerikhoIChannickRNSERAPHIN InvestigatorsMacitentan and morbidity and mortality in pulmonary arterial hypertensionN Engl J Med2013369980981823984728
   PubMed Web of Science ®Google Scholar
• DingemanseJSidhartaPNMaddreyWCRubinLJMickailHEfficacy, safety and clinical pharmacology of macitentan in comparison to other endothelin receptor antagonists in the treatment of pulmonary arterial hypertensionExpert Opin Drug Saf201413339140524261583
   PubMed Web of Science ®Google Scholar
• SidhartaPNTreiberADingemanseJClinical pharmacokinetics and pharmacodynamics of the endothelin receptor antagonist macitentanClin Pharmacokinet201554545747125860376
   PubMed Web of Science ®Google Scholar
• SidhartaPNvan GiersbergenPLMDingemanseJSafety, tolerability, pharmacokinetics, and pharmacodynamics of macitentan, an endothelin receptor antagonist, in an ascending multiple-dose study in healthy subjectsJ Clin Pharmacol201353111131113823900878
   PubMed Web of Science ®Google Scholar
• US Food and Drug AdministrationUS Food and Drug Administration, Center for Drug Evaluation and Research (CDER): Guidance for Industry: E14 Clinical Evaluation of QT/QTc Interval Prolongation and Proarrhythmic Potential for Nonantiarrhythmic Drugs – Questions and Answers (R3)Silver Spring, MD6201710201715507416
   Google Scholar
• GoughKHutchisonMKeeneOAssessment of dose proportionality: report from the statisticians in the pharmaceutical industry/pharmacokinetics UK joint working PartyDrug Inf J199529310391048
   Google Scholar
• KrumHViskoperRJLacourciereYBuddeMCharlonVThe effect of an endothelin-receptor antagonist, bosentan, on blood pressure in patients with essential hypertension. Bosentan Hypertension InvestigatorsN Engl J Med1998338127847919504938
   PubMed Web of Science ®Google Scholar
• PackerMMcMurrayJJVKrumHENABLE Investigators and CommitteesLong-term effect of endothelin receptor antagonism with bosentan on the morbidity and mortality of patients with severe chronic heart failure: primary results of the enable trialsJACC Heart Fail20175531732628449795
   PubMed Web of Science ®Google Scholar
• WeberMABlackHBakrisGA selective endothelin-receptor antagonist to reduce blood pressure in patients with treatment-resistant hypertension: a randomised, double-blind, placebo-controlled trialLancet200937496991423143119748665
   PubMed Web of Science ®Google Scholar
• BlackHRBakrisGLWeberMAEfficacy and safety of darusentan in patients with resistant hypertension: results from a randomized, double-blind, placebo-controlled dose-ranging studyJ Clin Hypertens (Greenwich)200791076076917917503
   PubMedGoogle Scholar
• StevensLAViswanathanGWeinerDEChronic kidney disease and end-stage renal disease in the elderly population: current prevalence, future projections, and clinical significanceAdv Chronic Kidney Dis201017429330120610356
   PubMed Web of Science ®Google Scholar
• EpsteinBJEfficacy and safety of darusentan: a novel endothelin receptor antagonistAnn Pharmacother20084271060106918523233
   PubMed Web of Science ®Google Scholar
• LeenenFHFourneyANotmanGTannerJPersistence of anti-hypertensive effect after “missed doses” of calcium antagonist with long (amlodipine) vs short (diltiazem) elimination half-lifeBr J Clin Pharmacol199641283888838433
   PubMed Web of Science ®Google Scholar
• BrambillaGBombelliMSeravalleGPrevalence and clinical characteristics of patients with true resistant hypertension in central and eastern Europe: data from the BP-CARE studyJ Hypertens201331102018202423838657
   PubMed Web of Science ®Google Scholar
• DaughertySLPowersJDMagidDJIncidence and prognosis of resistant hypertension in hypertensive patientsCirculation2012125131635164222379110
   PubMed Web of Science ®Google Scholar
• WetzelsJFKiemeneyLASwinkelsDWWillemsHLden HeijerMAge- and gender-specific reference values of estimated GFR in z: the Nijmegen Biomedical StudyKidney Int200772563263717568781
   PubMed Web of Science ®Google Scholar
• LöfflerBMBreuVClozelMEffect of different endothelin receptor antagonists and of the novel non-peptide antagonist Ro 46-2005 on endothelin levels in rat plasmaFEBS Lett19933331–21081108224145
   PubMed Web of Science ®Google Scholar
• IglarzMBinkertCMorrisonKPharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonistJ Pharmacol Exp Ther2008327373674518780830
   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 Pharmacol201566433233725992919
   PubMed Web of Science ®Google Scholar
• KakokiMHirataYHayakawaHEffects of hypertension, diabetes mellitus, and hypercholesterolemia on endothelin type B receptor-mediated nitric oxide release from rat kidneyCirculation19999991242124810069794
   PubMed Web of Science ®Google Scholar
• EMAAssessment Report. Opsumit. Procedure N° Emea/H/C/002697/00002013 Available From: https://www.ema.europa.eu/en/documents/assessment-report/opsumit-epar-public-assessment-report_en.pdfAccessed December 6, 2018
   Google Scholar
• GoddardJJohnstonNRHandMFEndothelin-A receptor antagonism reduces blood pressure and increases renal blood flow in hypertensive patients with chronic renal failure: a comparison of selective and combined endothelin receptor blockadeCirculation200410991186119314981006
   PubMed Web of Science ®Google Scholar
• BakrisGLLindholmLHBlackHRDivergent results using clinic and ambulatory blood pressures: report of a darusentan-resistant hypertension trialHypertension201056582483020921430
   PubMed Web of Science ®Google Scholar
• ScienceGSecond pivotal Phase III study of Gilead’s darusentan for resistant hypertension misses primary endpoints2009 Available from: www.gilead.comAccessed December 6, 2018
   Google Scholar