213
Views
3
CrossRef citations to date
0
Altmetric
Drug Profiles

Macitentan for the treatment of pulmonary arterial hypertension

&

References

  • Simonneau G, Gatzoulis MA, Adatia I, et al. Updated clinical classification of pulmonary hypertension. J Am Coll Cardiol 2013;62(25):D34-41
  • Humbert M, Morrell NW, Archer SL, et al. Cellular and molecular pathobiology of pulmonary arterial hypertension. J Am Coll Cardiol 2004;43(12):13S-24S
  • Sitbon O, Morrell NW. Pathways in pulmonary arterial hypertension: the future is here. Eur Respir Rev 2012;21(126):321-7
  • Rubin LJ. Primary pulmonary hypertension. N Engl J Med 1997;336:111-17
  • Task Force for Diagnosis and Treatment of Pulmonary Hypertension of European Society of Cardiology (ESC), European Respiratory Society (ERS), and International Society of Heart and Lung Transplantation (ISHLT). Galie N, Hoepper MM, Humbert M, et al. Guidelines for the diagnosis and treatment of pulmonary hypertension. Eur Respir J 2009;34(6):1219-63
  • 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;328:1732-9
  • Davie N, Haleen SJ, Upton PD, et al. ET(A) and ET(B) receptors modulate the proliferation of pulmonary artery smooth muscle cells. Am J Respir Crit Care Med 2002;165(3):398-405
  • Dupuis J, Hoepper M. Endothelin receptor antagonists in pulmonary arterial hypertension. Eur Respir J 2008;31(2):407-15
  • Cardillo C, Kilcoyne CM, Waclawiw M, et al. Role of endothelin in the increased vascular tone of patients with essential hypertension. Hypertension 1999;33(2):753-8
  • Sauvageau S, Thorin E, Caron A, Dupuis J. Evaluation of endothelin-1-induced pulmonary vasoconstriction following myocardial infarction. Exp Biol Med (Maywood) 2006;231(6):840-6
  • Sauvageau S, Thorin E, Caron A, Dupuis J. Endothelin-1-induced pulmonary vasoreactivity is regulated by ETA and ETB receptor interactions. J Vasc Res 2007;44:375-81
  • Rubin LJ, Badesch DB, Barst RJ, et al. Bosentan therapy for pulmonary arterial hypertension. N Engl J Med 2002;346:896-903
  • Galiè N, Olschewski H, Oudiz RJ, et al. Ambrisentan for the treatment of pulmonary arterial hypertension: results of the ambrisentan in pulmonary arterial hypertension, randomised, double-blind, placebo-controlled, multicenter, efficacy (ARIES) study 1 and 2. Circulation 2008;117(23):3010-19
  • Galiè N, Rubin LJ, Hoepper M, et al. Treatment of patients with mildly symptomatic pulmonary arterial hypertension with bosentan (EARLY study): a double-blind, randomised controlled trial. Lancet 2008;371(9630):2093-100
  • Simonneau G, Galie N, Jansa P, et al. Long-term results from the EARLY study of bosentan in WHO functional class II pulmonary arterial hypertension patients. Int J Cardiol 2014;172(2):332-9
  • Lavelle A, Sugrue R, Lawler G, et al. Sitaxentan-induced hepatic failure in two patients with pulmonary arterial hypertension. Eur Respir J 2009;34:770-1
  • Fattinger K, Funk C, Pantze M, et al. The endothelin antagonist bosentan inhibits the canalicular bile salt export pump: a potential mechanism for hepatic adverse reactions. Clin Pharmacol Ther 2001;69:223-31
  • Comellas AP, Briva A, Dada LA, et al. Endothelin-1 impairs alveolar epithelial function via endothelial ETB receptor. Am J Resp Crit Care Med 2009;179(2):113-22
  • Bolli MH, Boss C, Binkert C, et al. The discovery of a N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N’-propylsulfamide (Macitentan), an orally active, potent, dual endothelin receptor antagonist. J Med Chem 2012;55(17):7849-61
  • Dingemanse J, Sidharta PN, Maddrey WC, et al. 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(3):391-405
  • Iglarz M, Binkert C, Morrison K, et al. Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. J Pharmacol Exp Ther 2008;327(3):736-45
  • Gatfield J, Grandjean CM, Sasse T, et al. Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor anatagonists in pulmonary arterial smooth muscle cells. PLoS One 2012;7(10):1-11
  • Iglarz M, Bossu A, Wanner D. Comparison of pharmacological activity of macitentan and bosentan in preclinical models of systemic and pulmonary hypertension. Life Sci 2014. [Epub ahead of print]
  • Sidharta PN, Giersbergen P, Halabi P, Dingemanse J. Macitentan: entry into humans study with a new endothelin receptor antagonist. Eur J Clin Pharmacol 2011;67:977-84
  • Sidharta PN, van Giersbergen PL, Dingemanse J. Safety, tolerability, pharmacokinetics and pharmacodynamics of macitentan, an endothelin receptor antagonist, in an ascending multiple dose study in healthy subjects. J Clin Pharmacol 2013;53(11):1131-8
  • Atsmon J, Dingemanse J, Shaikevich D, et al. Investigation of the effects of ketoconazole on the pharmacokinetics of macitentan, a novel dual endothelin receptor antagonist, in healthy subjects. Clin Pharmacokinet 2013;52(8):685-92
  • Bruderer S, Hopfgartner GR, Seiberling M, et al. Absorption, distribution, metabolism, and excretion of macitentan, a dual endothelin receptor antagonist, in humans. Xenobiotica 2012;42(9):901-10
  • Raghu G, Million-Rousseau R, Morganti A, et al. Macitentan for the treatment of idiopathic pulmonary fibrosis: the randomised controlled MUSIC trial. Eur Respir J 2013;42(6):1622-32
  • Pulido T, Adzerikho I, Channick RN, et al. Macitentan and morbidity and mortality in pulmonary arterial hypertension. N Engl J Med 2013;369:809-18
  • Patel T, McKeage K. Macitentan: first Global Approval. Drugs 2014;74:127-33
  • Thompson CA. Macitentan approved by FDA to delay progression of PAH. Am J Health-Syst Pharm 2013;70:2054
  • Weiss J, Theile D, Ruppell MA, et al. Interaction profile of macitentan, a new non-selective sendothelin-1 receptor antagonist, in vitro. Eur J Pharmacol 2013;701(1-3):168-75
  • Bruderer S, Aanismaa P, Homery MC, et al. Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue targeting dual endothelin receptor antagonist. AAPS J 2012;14(1):68-78
  • Sidharta PN, Lindegger N, Ulc I, Dingemanse J. Pharmacokinetics of the novel dual endothelin receptor antagonist macitentan in subjects with renal or hepatic impairment. J Clin Pharmacol 2014;54(3):291-300
  • Sidharta PN, van Giersbergen PL, Wolzt M, et al. Lack of clinically relevant pharmacokinetic interactions between the dual endothelin receptor antagonist macitentan and sildenafil in healthy subjects. Am J Respir Crit Care Med 2012;185:A4802
  • Sidharta PN, Dietrich H, Dingemanse J. Investigation of the effect of macitentan on the pharmacokinetics and pharmacodynamics of warfarin healthy male subjects. Br J Clin Pharmacol 2009;68:788-9

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.