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Review

Safety and tolerability of macitentan in the management of pulmonary arterial hypertension: an update

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Pages 71-85 | Published online: 03 Sep 2019

References

  • Simonneau G, Gatzoulis MA, Adatia I, et al. Updated clinical classification of pulmonary hypertension. J Am Coll Cardiol. 2013;62:D34–D41. doi:10.1016/j.jacc.2013.10.02924355639
  • McGoon MD, Benza RL, Escribano-Subias P, et al. Pulmonary arterial hypertension. J Am Coll Cardiol. 2013;62:D51–D59. doi:10.1016/j.jacc.2013.10.02324355642
  • Galiè N, Humbert M, Vachiery, JL, et al. 2015 ESC/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 Heart J. 2016;37:67–119.26320113
  • Hoeper MM, Wedzicha JA, Iversen M, et al. Mortality in pulmonary arterial hypertension: prediction by the 2015 European pulmonary hypertension guidelines risk stratification model. Eur Respir J. 2017;50:1700740. doi:10.1183/13993003.00711-201728775047
  • Pulido T, Adzerikho I, Channick RN, et al. Macitentan and morbidity and mortality in pulmonary arterial hypertension. N Engl J Med. 2013;369:809–818. doi:10.1056/NEJMoa121391723984728
  • Rubin LJ. Endothelin receptor antagonists for the treatment of pulmonary artery hypertension. Life Sci. 2012;91:517–521. doi:10.1016/j.lfs.2012.07.03322884806
  • Yanagisawa M, Inoue A, Takuwa Y, Mitsui Y, Kobayashi M, Masaki T. The human preproendothelin-1 gene: possible regulation by endothelial phosphoinositide turnover signaling. J Cardiovasc Pharmacol. 1989;13:S13–S17.
  • Clarke J, Benjamin NI, Larkin SW, Webb DJ, Davies GJ, Maseri A. Endothelin is a potent long-lasting vasoconstrictor in men. Am J Physiol. 1989;257:H2033–H2035. doi:10.1152/ajpheart.1989.257.6.H20332690644
  • Channick RN, Sitbon O, Barst RJ, Manes A, Rubin LJ. Endothelin receptor antagonists in pulmonary arterial hypertension. J Am Coll Cardiol. 2004;43:S62–S67. doi:10.1016/j.jacc.2004.02.042
  • Stewart D, Levy R, Cernacek P, Langleben D. Increased plasma endothelin-1 in pulmonary hypertesnion: marker or mediator of disease. Ann Intern Med. 1991;114:464–469. doi:10.7326/0003-4819-114-6-4641994793
  • Giaid A, Yanagisawa M, Langleben D, et al. Expression of endothelin-1 in the lungs of patients with pulmonary hypertension. N Engl J Med. 1993;328:1732–1739. doi:10.1056/NEJM1993061732824028497283
  • Davie N, Haleen SJ, Upton PD. et al. ET(A) and ET(B) receptors modulate the proliferation of human pulmonary artery smooth muscle cells. Am J Respir Crit Care Med. 2002;165:398–405. doi:10.1164/ajrccm.165.8.210610411818328
  • Wilson DW, Segall HJ, Pan LC, Lamé MW, Estep JE, Morin D. Mechanisms and pathology of monocrotaline pulmonary toxicity. Crit Rev Toxicol. 1992;22:307–325. doi:10.3109/104084492091463111489509
  • Jasmin J-F, Lucas M, Cernacek P, Dupuis J. Effectiveness of a nonselective ET A/B and a selective ET A antagonist in rats with monocrotaline-induced pulmonary hypertension. Circulation. 2001;103:314–318. doi:10.1161/01.CIR.103.2.31411208695
  • Lai Y-C, Potoka KC, Champion HC, Mora AL, Gladwin MT. Pulmonary arterial hypertension: the clinical syndrome. Circ Res. 2014;115:115–130. doi:10.1161/CIRCRESAHA.115.30114624951762
  • Selej M, Romero AJ, Channick RN, Clozel M. Development of macitentan for the treatment of pulmonary arterial hypertension: macitentan for the treatment of pulmonary arterial hypertension. Ann N Y Acad Sci. 2015;1358:68–81. doi:10.1111/nyas.1285626291180
  • Hong IS. Macitentan for the treatment of pulmonary arterial hypertension. Ann Pharmacother. 2014;48:538–547. doi:10.1177/1060028013518900
  • Iglarz M, Bossu A, Wanner D, et al. Comparison of pharmacological activity of macitentan and bosentan in preclinical models of systemic and pulmonary hypertension. Life Sci. 2014;118:333–339. doi:10.1016/j.lfs.2014.02.01824582812
  • Sidharta PN, van Giersbergen PLM, Halabi A, Dingemanse J. Macitentan: entry-into-humans study with a new endothelin receptor antagonist. Eur J Clin Pharmacol. 2011;67:977–984. doi:10.1007/s00228-011-1043-221541781
  • Sidharta PN, van Giersbergen PLM, Dingemanse J. Safety, tolerability, pharmacokinetics, and pharmacodynamics of macitentan, an endothelin receptor antagonist, in an ascending multiple-dose study in healthy subjects: the journal of clinical pharmacology. J Clin Pharmacol. 2013; n/a-n/a. doi:10.1002/jcph.152
  • Paul GA, Gibbs JSR, Boobis AR, Abbas A, Wilkins MR. Bosentan decreases the plasma concentration of sildenafil when coprescribed in pulmonary hypertension. Br J Clin Pharmacol. 2005;60:107–112. doi:10.1111/j.1365-2125.2005.02383.x15963102
  • Burgess G, Hoogkamer H, Collings L, Dingemanse J. Mutual pharmacokinetic interactions between steady-state bosentan and sildenafil. Eur J Clin Pharmacol. 2008;64:43–50. doi:10.1007/s00228-007-0408-z18040672
  • Sidharta PN, van Giersbergen PLM, Wolzt M, Dingemanse J. Investigation of mutual pharmacokinetic interactions between macitentan, a novel endothelin receptor antagonist, and sildenafil in healthy subjects: pharmacokinetic interactions between macitentan and sildenafil. Br J Clin Pharmacol. 2014;78:1035–1042. doi:10.1111/bcp.1244724962473
  • Raghu G, Million-Rousseau R, Morganti A, Perchenet L, Behr J. Macitentan for the treatment of idiopathic pulmonary fibrosis: the randomised controlled MUSIC trial. Eur Respir J. 2013;42:1622–1632. doi:10.1183/09031936.0010461223682110
  • Channick RN, Delcroix M, Ghofrani HA, et al. Effect of macitentan on hospitalizations. JACC Heart Fail. 2015;3:1–8. doi:10.1016/j.jchf.2014.07.01325457902
  • Galiè N, Jansa P, Pulido T, et al. SERAPHIN haemodynamic substudy: 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 hypertension. Eur Heart J. 2017;38:1147–1155. doi:10.1093/eurheartj/ehx02528329315
  • Mehta S, Sastry BKS, Souza R, et al. Macitentan improves health-related quality of life for patients with pulmonary arterial hypertension. Chest. 2017;151:106–118. doi:10.1016/j.chest.2016.08.147327671974
  • Vanhoof JMM, Page RLEA, Ambardekar AV, Brieke A, Lindenfeld J. Emotional symptoms and quality of life in patients with pulmonary arterial hypertension. J Heart Lung Transplant. 2014;33:800–808. doi:10.1016/j.healun.2014.08.02224854567
  • Vachiéry J-L, Delcroix M, Al-Hiti H, et al. Macitentan in pulmonary hypertension due to left ventricular dysfunction. Eur Respir J. 2018;51:1701886. doi:10.1183/13993003.01886-201729437943
  • Ghofrani H-A, Casarin A, Ely EW, et al. Macitentan for the treatment of inoperable chronic thromboembolic pulmonary hypertension (MERIT-1): results from the multicentre, phase 2, randomised, double-blind, placebo-controlled study. Lancet Respir Med. 2017;5:785–794. doi:10.1016/S2213-2600(17)30234-528919201
  • Ghofrani H-A, D’Armini AM, Grimminger F, et al. Riociguat for the treatment of chronic thromboembolic pulmonary hypertension. N Engl J Med. 2013;369:319–329. doi:10.1056/NEJMoa120965723883377
  • Galiè N, Beghetti M, Gatzoulis MA, et al. Bosentan therapy in patients with eisenmenger syndrome: a multicenter, double-blind, randomized, placebo-controlled study. Circulation. 2006;114:48–54. doi:10.1161/CIRCULATIONAHA.106.63071516801459
  • Gatzoulis MA, Landzberg M, Beghetti M, et al. Evaluation of macitentan in patients with Eisenmenger syndrome. Circulation. 2019;139:51–63. doi:10.1161/CIRCULATIONAHA.118.03357530586694
  • Duo-Ji -M-M, Long Z-W. Comparative efficacy and acceptability of endothelin receptor antagonists for pulmonary arterial hypertension: a network meta-analysis. Int J Cardiol. 2017;234:90–98. doi:10.1016/j.ijcard.2016.12.09228233631
  • Dingemanse J, Sidharta PN, Maddrey WC, Rubin LJ, Mickail H. Efficacy, safety and clinical pharmacology of macitentan in comparison to other endothelin receptor antagonists in the treatment of pulmonary arterial hypertension. Expert Opin Drug Saf. 2014;13:391–405. doi:10.1517/14740338.2014.85967424261583
  • Davila C, Monaco T. Safety, efficacy, and clinical utility of macitentan in the treatment of pulmonary arterial hypertension. Drug Des Devel Ther. 2016;1675. doi:10.2147/DDDT.S88612
  • Wei A, Gu Z, Li J, et al. Clinical adverse effects of endothelin receptor antagonists: insights from the meta‐analysis of 4894 patients from 24 randomized double‐blind placebo‐controlled clinical trials. J Am Heart Assoc. 2016;5. doi:10.1161/JAHA.116.003896
  • Trow T, Fares W, Kholdani C. Macitentan for the treatment of pulmonary arterial hypertension. Vasc Health Risk Manag. 2014;665. doi:10.2147/VHRM.S3390425473292
  • Vercauteren M, Strasser D, Vezzali E. et al. Vasopressin in involved in endothelin receptor antagonist-induced fluid retention in rat. Differential effect of selective ETA and dual ETA/ETB receptor antagonists. Eur Respir J. 2012;40:716s. doi:10.1183/09031936.00213711
  • Ge Y, Bagnall A, Stricklett PK, Webb D, Kotelevtsev Y, Kohan DE. Combined knockout of collecting duct endothelin A and B receptors causes hypertension and sodium retention. Am J Physiol- Ren Physiol. 2008;295:F1635–F1640. doi:10.1152/ajprenal.90279.2008
  • Shapiro S, Chun L, Patton KK, Matsushita MM, Page RL, Raskind WH. Frequency of edema in patients with pulmonary arterial hypertension receiving ambrisentan. Am J Cardiol. 2012;110:1373–1377. doi:10.1016/j.amjcard.2012.07.03322858181
  • Gabbay E, Fraser J, McNeil K. Review of bosentan in the management of pulmonary arterial hypertension. Vasc Health Risk Manag. 2007;3:887–900.18200808
  • Center for Drug Evaluation And Research; Approval Package for Macitentan. Available from: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/204410Orig1s000Approv.pdf. Accessed December 2, 2018.
  • OPsumit users registry - full text view - ClinicalTrials.gov. Available from: https://clinicaltrials.gov/ct2/show/NCT02126943. Accessed 122, 2018.
  • Kim NH, Bergmark BA, Zelniker TA, et al. OPUS registry: safety and tolerability of macitentan in a real-world setting. J Heart Lung Transplant. 2017;36:S20–S21. doi:10.1016/j.healun.2017.06.015
  • Kim NH, Chin KM, Muros-Le Rouzic E. et al. OPsumit® USers Registry (OPUS): insights into the safety and tolerability of Opsumit® | D54. CLINICAL PULMONARY HYPERTENSION. Am J Respir Crit Care Med. 2016;A7396.
  • Chin KM, Channick RN, Kim NH, et al. OPUS registry: treatment patterns with macitentan in patients with pulmonary arterial hypertension. Am J Respir Crit Care Med. 2017;195:A2299.
  • Chin KM, Kim N, Channick R, Muros-Le Rouzic E, Selej M, McLaughlin V. OPUS registry: treatment patterns and safety of macitentan in patients with Pulmonary Arterial Hypertension Associated with Systemic Sclerosis (PAH-SSc). Chest. 2017;152:A999–A1000. doi:10.1016/j.chest.2017.08.1036
  • McLaughlin VV, Channick R, Chin KM, et al. The OPSUMIT Users Registry: a Gender Subgroup Analysis of Patient Characetistics, Treatment Patterns and Survival in Pulmonary Arterial Hypertension. J Am Coll Cardiol. 2018;71(Supplement). doi:10.1016/S0735-1097(18)32493-8
  • FDA Opsumit Package Insert. Available from: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204410s000lbl.pdf. Accessed 124, 2018.
  • Monograph AO. Available from: https://www1.actelion.com/documents/ca/ca-opsumit-procuct-monograph-en.pdf. Accessed 124, 2018.
  • Safdar Z, Thakur A, Frost A. Tolerability of switch to macitentan from bosentan in pulmonary arterial hypertension. South Med J. 2017;110:223–228. doi:10.14423/SMJ.000000000000073828257550
  • Blok I, van Riel AC, van Dijk AP, Mulder BJ, Bouma BJ. From bosentan to macitentan for pulmonary arterial hypertension and adult congenital heart disease: further improvement? Int J Cardiol. 2017;227:51–52. doi:10.1016/j.ijcard.2016.11.21127846462
  • Herbert S, Gin-Sing W, Howard L, Tulloh RMR. Early experience of macitentan for pulmonary arterial hypertension in adult congenital heart disease. Heart Lung Circ. 2017;26:1113–1116. doi:10.1016/j.hlc.2016.12.01128237536
  • Jansa P, Pulido T. Macitentan in pulmonary arterial hypertension: a focus on combination therapy in the SERAPHIN trial. Am J Cardiovasc Drugs. 2018;18:1–11. doi:10.1007/s40256-017-0255-y29280064
  • The efficacy and safety of initial triple versus initial dual oral combination therapy in patients with newly diagnosed pulmonary arterial hypertension - full text view - ClinicalTrials.gov. Available from: https://clinicaltrials.gov/ct2/show/NCT02558231. Accessed 1127, 2018.