Endothelin receptor antagonists in pulmonary arterial hypertension

European Respiratory Journal

Volumn 31, Issue 2, 2008, Pages 407-415

  Dupuis, J ^a,b   Hoeper, M M ^c  

^a MONTREAL HEART INSTITUTE   (Canada)

^b UNIVERSITÉ DE MONTRÉAL   (Canada)

^c HANNOVER MEDICAL SCHOOL   (Germany)

Author keywords

Endothelin; Endothelin receptor antagonists; Hypertension; Pulmonary

Indexed keywords

AMBRISENTAN; BOSENTAN; ENDOTHELIN; ENDOTHELIN 1; ENDOTHELIN RECEPTOR; ILOPROST; PLACEBO; PROSTACYCLIN; SILDENAFIL; SITAXSENTAN; WARFARIN; ENDOTHELIN A RECEPTOR; ENDOTHELIN B RECEPTOR; ISOXAZOLE DERIVATIVE; PHENYLPROPIONIC ACID DERIVATIVE; PYRIDAZINE DERIVATIVE; SULFONAMIDE; THIOPHENE DERIVATIVE;

AMINOTRANSFERASE BLOOD LEVEL; CLINICAL TRIAL; DOSE RESPONSE; DRUG ACTIVITY; DRUG ANTAGONISM; DRUG BLOOD LEVEL; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG WITHDRAWAL; HEADACHE; HUMAN; LIVER DISEASE; LIVER TOXICITY; LUNG FUNCTION; NONHUMAN; PERIPHERAL EDEMA; PRIORITY JOURNAL; PULMONARY HYPERTENSION; REVIEW; SIDE EFFECT; TREATMENT OUTCOME; ANIMAL; HOSPITALIZATION; MORTALITY; PHASE 3 CLINICAL TRIAL; PROGNOSIS; RANDOMIZED CONTROLLED TRIAL; SURVIVAL RATE;

ANIMALS; CLINICAL TRIALS, PHASE III AS TOPIC; HUMANS; HYPERTENSION, PULMONARY; ISOXAZOLES; PHENYLPROPIONATES; PROGNOSIS; PYRIDAZINES; RANDOMIZED CONTROLLED TRIALS AS TOPIC; RECEPTOR, ENDOTHELIN A; RECEPTOR, ENDOTHELIN B; RECEPTORS, ENDOTHELIN; SEVERITY OF ILLNESS INDEX; SULFONAMIDES; SURVIVAL RATE; THIOPHENES; TREATMENT OUTCOME;

EID: 40649084619     PISSN: 09031936     EISSN: 13993003     Source Type: Journal    
DOI: 10.1183/09031936.00078207     Document Type: Review

References (80)

1. Hoeper MM, Dinh-Xuan AT. Pulmonary hypertension: basic concepts and practical management. Eur Respir J 2008; 31: 236-237.
2. Yanagisawa M, Kurihara H, Kimura S, et al. A novel potent vasoconstrictor peptide produced by vascular endothelial cells. Nature 1988; 332: 411-415.
3. Markewitz BA, Farrukh IS, Chen Y, Li Y, Michael JR. Regulation of endothelin-1 synthesis in human pulmonary arterial smooth muscle cells. Effects of transforming growth factor-β and hypoxia. Cardiovasc Res 2001; 49: 200-206.
4. Shi-Wen X, Chen Y, Denton CP, et al. Endothelin-1 promotes myofibroblast induction through the ETA receptor via a rac/phosphoinositide 3-kinase/Akt-dependent pathway and is essential for the enhanced contractile phenotype of fibrotic fibroblasts. Mol Biol Cell 2004; 15: 2707-2719.
5. Boulanger C, Luscher TF. Release of endothelin from the porcine aorta. Inhibition by endothelium-derived nitric oxide. J Clin Invest 1990; 85: 587-590.
6. Takahashi M, Matsushita Y, Iijima Y, Tanzawa K. Purification and characterization of endothelin-converting enzyme from rat lung. J Biol Chem 1993; 268: 21394-21398.
7. Matsumoto H, Suzuki N, Onda H, Fujino M. Abundance of endothelin-3 in rat intestine, pituitary gland and brain. Biochem Biophys Res Commun 1989; 164: 74-80.
8. Firth JD, Ratcliffe PJ. Organ distribution of the three rat endothelin messenger RNAs and the effects of ischemia on renal gene expression. J Clin Invest 1992; 90: 1023-1031.
9. Dupuis J, Goresky CA, Stewart DJ. Pulmonary removal and production of endothelin in the anesthetized dog. J Appl Physiol 1994; 76: 694-700.
10. Dupuis J, Stewart DJ, Cernacek P, Gosselin G. Human pulmonary circulation is an important site for both clearance and production of endothelin-1. Circulation 1996; 94: 1578-1584.
11. Masuda Y, Miyazaki H, Kondoh M, et al. Two different forms of endothelin receptors in rat lung. FEBS Lett 1989; 257: 208-210.
12. Migneault A, Sauvageau S, Villeneuve L, et al. Chronically elevated endothelin levels reduce pulmonary vascular reactivity to nitric oxide. Am J Respir Crit Care Med 2005; 171: 506-513.
13. Davenport AP. International Union of Pharmacology. XXIX. Update on endothelin receptor nomenclature. Pharmacol Rev 2002; 54: 219-226.
14. Shi-Wen X, Rodriguez-Pascual F, Lamas S, et al. Constitutive ALK5-independent c-Jun N-terminal kinase activation contributes to endothelin-1 overexpression in pulmonary fibrosis: evidence of an autocrine endothelin loop operating through the endothelin A and B receptors. Mol Cell Biol 2006; 26: 5518-5527.
15. Sauvageau S, Thorin E, Caron A, Dupuis J. Evaluation of endothelin-1-induced pulmonary vasoconstriction following myocardial infarction. Exp Biol Med (Maywood) 2006; 231: 840-846.
16. B receptor interactions. J Vasc Res 2007; 44: 375-381.
17. Gregan B, Jurgensen J, Papsdorf G, et al. Ligand-dependent differences in the internalization of endothelin A and endothelin B receptor heterodimers. J Biol Chem 2004; 279: 27679-27687.
18. Gregan B, Schaefer M, Rosenthal W, Oksche A. Fluorescence resonance energy transfer analysis reveals the existence of endothelin-A and endothelin-B receptor homodimers. J Cardiovasc Pharmacol 2004; 44: S30-S33.
19. B receptor heterodimer. Cell Mol Neurobiol 2002; 22: 207-226.
20. Stannard C, Lehenkari P, Godovac-Zimmermann J. Functional diversity of endothelin pathways in human lung fibroblasts may be based on structural diversity of the endothelin receptors. Biochemistry 2003; 42: 13909-13918.
21. Knott PG, D'Aprile AC, Henry PJ, Hay DW, Goldie RG. Receptors for endothelin-1 in asthmatic human peripheral lung. Br J Pharmacol 1995; 114: 1-3.
22. Goldie RG, D'Aprile AC, Self GJ, Rigby PJ, Henry PJ. The distribution and density of receptor subtypes for endothelin-1 in peripheral lung of the rat, guinea-pig and pig. Br J Pharmacol 1996; 117: 729-735.
23. B receptors modulate the proliferation of human pulmonary artery smooth muscle cells. Am J Respir Crit Care Med 2002; 165: 398-405.
24. B receptor-mediated contraction in human pulmonary resistance arteries. Br J Pharmacol 1996; 119: 1125-1130.
25. B receptor-mediated contraction of human and rat pulmonary resistance arteries and the effect of pulmonary hypertension on endothelin responses in the rat. J Cardiovasc Pharmacol 1995; 26: Suppl. 3, S169-S176.
26. B antagonists on responses to ET-1 in human small muscular pulmonary arteries. Pulm Pharmacol Ther 1998; 11: 147-149.
27. McCulloch KM, Docherty C, MacLean MR. Endothelin receptors mediating contraction of rat and human pulmonary resistance arteries: effect of chronic hypoxia in the rat. Br J Pharmacol 1998; 123: 1621-1630.
28. Hirata Y, Emori T, Eguchi S, et al. Endothelin receptor subtype B mediates synthesis of nitric oxide by cultured bovine endothelial cells. J Clin Invest 1993; 91: 1367-1373.
29. Lal H, Woodward B, Williams KI. Investigation of the contributions of nitric oxide and prostaglandins to the actions of endothelins and sarafotoxin 6c in rat isolated perfused lungs. Br J Pharmacol 1996; 118: 1931-1938.
30. B receptor in the regulation of pulmonary vascular tone. Pulm Pharmacol Ther 2000; 13: 135-140.
31. Muramatsu M, Oka M, Morio Y, Soma S, Takahashi H, Fukuchi Y. Chronic hypoxia augments endothelin-B receptor-mediated vasodilation in isolated perfused rat lungs. Am J Physiol 1999; 276: L358-L364.
32. B receptor, NADPH oxidase and caveolin-1. Br J Pharmacol 2005; 145: 323-333.
33. Hocher B, Schwarz A, Fagan KA, et al. Pulmonary fibrosis and chronic lung inflammation in ET-1 transgenic mice. Am J Respir Cell Mol Biol 2000; 23: 19-26.
34. Battistini B, Dussault P. Blocking of the endothelin system: the development of receptor antagonists. Pulm Pharmacol Ther 1998; 11: 97-112.
35. Vatter H, Seifert V. Ambrisentan, a non-peptide endothelin receptor antagonist. Cardiovasc Drug Rev 2006; 24: 63-76.
36. Michel RP, Langleben D, Dupuis J. The endothelin system in pulmonary hypertension. Can J Physiol Pharmacol 2003; 81: 542-554.
37. 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.
38. Bressollette E, Dupuis J, Bonan R, Doucet S, Cernacek P, Tardif JC. Intravascular ultrasound assessment of pulmonary vascular disease in patients with pulmonary hypertension. Chest 2001; 120: 809-815.
39. Rubens C, Ewert R, Halank M, et al. Big endothelin-1 and endothelin-1 plasma levels are correlated with the severity of primary pulmonary hypertension. Chest 2001; 120: 1562-1569.
40. Dupuis J, Cernacek P, Tardif JC, et al. Reduced pulmonary clearance of endothelin-1 in pulmonary hypertension. Am Heart J 1998; 135: 614-620.
41. B receptors. J Appl Physiol 1996; 81: 1510-1515.
42. Langleben D, Dupuis J, Langleben I, et al. Etiology-specific endothelin-1 clearance in human precapillary pulmonary hypertension. Chest 2006; 129: 689-695.
43. A receptor blockade improves nitric oxide-mediated vasodilation in monocrotaline-induced pulmonary hypertension. Circulation 1998; 97: 2169-2174.
44. A-receptor antagonist LU 135252 prevents the progression of established pulmonary hypertension induced by monocrotaline in rats. J Cardiovasc Pharmacol 1999; 4: 33-39.
45. A receptor antagonist (+)-(S)-2-(4,6-dimethoxy-pyrimidin-2-yloxy)- 3-methoxy-3,3-diphenylpropionic acid (LU 135252) prevents the development of pulmonary hypertension and endothelial metabolic dysfunction in monocrotaline-treated rats. J Pharmacol Exp Ther 1997; 282: 1312-1318.
46. Williamson DJ, Wallman LL, Jones R, et al. Hemodynamic effects of bosentan, an endothelin receptor antagonist, in patients with pulmonary hypertension. Circulation 2000; 102: 411-418.
47. Oudiz RJ, Torres F, Frost AE, et al. ARIES-1: a placebo-controlled efficacy and safety study of Ambrisentan in patients with pulmonary arterial hypertension. Chest 2006; 1:3:0: 121S.
48. Olschewski H, Galle N, Kramer M, Rubin LJ, the ARIES-2 study group. Ambrisentan improves exercise capacity and time to clinical worsening in patients with pulmonary arterial hypertension: results of the ARIES-2 study. Am J Respir Crit Care Med 2006; 173: A728.
49. Channick RN, Simonneau G, Sitbon O, et al. Effects of the dual endothelin-receptor antagonist bosentan in patients with pulmonary hypertension: a randomised placebo-controlled study. Lancet 2001; 358: 1119-1123.
50. Rubin LJ, Badesch DB, Barst RJ, et al. Bosentan therapy for pulmonary arterial hypertension. N Engl J Med 2002; 346: 896-903.
51. Humbert M, Barst RJ, Robbins IM, et al. Combination of bosentan with epoprostenol in pulmonary arterial hypertension: BREATHE-2. Eur Respir J 2004; 24: 353-359.
52. Barst RJ, Ivy D, Dingemanse J, et al. Pharmacokinetics, safety, and efficacy of bosentan in pediatric patients with pulmonary arterial hypertension. Clin Pharmacol Ther 2003; 73: 372-382.
53. Sitbon O, Gressin V, Speich R, et al. Bosentan for the treatment of human immunodeficiency virus-associated pulmonary arterial hypertension. Am J Respir Crit Care Med 2004; 170: 1212-1217.
54. Galie 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.
55. Barst RJ, Langleben D, Frost A, et al. Sitaxsentan therapy for pulmonary arterial hypertension. Am J Respir Crit Care Med 2004; 169: 441-447.
56. Barst RJ, Langleben D, Badesch D, et al. Treatment of pulmonary arterial hypertension with the selective endothelin-A receptor antagonist sitaxsentan. J Am Coll Cardiol 2006; 47: 2049-2056.
57. Humbert M, Segal ES, Kiely DG, Carlsen J, Schwierin B, Hoeper MM. Results of European post-marketing surveillance of bosentan in pulmonary hypertension. Eur Respir J 2007; 30: 338-344.
58. McLaughlin VV, Sitbon O, Badesch DB, et al. Survival with first-line bosentan in patients with primary pulmonary hypertension. Eur Respir J 2005; 25: 244-249.
59. Provencher S, Sitbon O, Humbert M, Cabrol S, Jais X, Simonneau G. Long-term outcome with first-line bosentan therapy in idiopathic pulmonary arterial hypertension. Eur Heart J 2006; 27: 589-595.
60. Sitbon O, McLaughlin VV, Badesch DB, et al. Survival in patients with class III idiopathic pulmonary arterial hypertension treated with first line oral bosentan compared with an historical cohort of patients started on intravenous epoprostenol. Thorax 2005; 60: 1025-1030.
61. Hoeper MM, Halank M, Marx C, et al. Bosentan therapy for portopulmonary hypertension. Eur Respir J 2005; 25: 502-508.
62. Hoeper M, Seyfarth HJ, Hoeffken G, et al. Experience with inhaled iloprost and bosentan in portopulmonary hypertension. Eur Respir J 2007; [Epub ahead of print PMID: 17652314].
63. Hoeper MM, Dinh-Xuan AT. Combination therapy for pulmonary arterial hypertension: still more questions than answers. Eur Respir J 2004; 24: 339-340.
64. Hoeper MM, Taha N, Bekjarova A, Gatzke R, Spiekerkoetter E. Bosentan treatment in patients with primary pulmonary hypertension receiving nonparenteral prostanoids. Eur Respir J 2003; 22: 330-334.
65. Seyfarth HJ, Pankau H, Hammerschmidt S, Schauer J, Wirtz H, Winkler J. Bosentan improves exercise tolerance and Tei index in patients with pulmonary hypertension and prostanoid therapy. Chest 2005; 128: 709-713.
66. Hoeper MM, Leuchte H, Halank M, et al. Combining inhaled iloprost with bosentan in patients with idiopathic pulmonary arterial hypertension. Eur Respir J 2006; 28: 691-694.
67. McLaughlin VV, Oudiz RJ, Frost A, et al. Randomized study of adding inhaled iloprost to existing bosentan in pulmonary arterial hypertension. Am J Respir Crit Care Med 2006; 174: 1257-1263.
68. Hoeper MM, Faulenbach C, Golpon H, Winkler J, Welte T, Niedermeyer J. Combination therapy with bosentan and sildenafil in idiopathic pulmonary arterial hypertension. Eur Respir J 2004; 24: 1007-1010.
69. Mathai SC, Girgis RE, Fisher MR, et al. Addition of sildenafil to bosentan monotherapy in pulmonary arterial hypertension. Eur Respir J 2007; 29: 469-475.
70. Hoeper MM. Observational trials in pulmonary arterial hypertension: low scientific evidence but high clinical value. Eur Respir J 2007; 29: 432-434.
71. Paul GA, Gibbs JS, 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.
72. Bonderman D, Nowotny R, Skoro-Sajer N, et al. Bosentan therapy for inoperable chronic thromboembolic pulmonary hypertension. Chest 2005; 128: 2599-2603.
73. Hoeper MM, Kramm T, Wilkens H, et al. Bosentan therapy for inoperable chronic thromboembolic pulmonary hypertension. Chest 2005; 128: 2363-2367.
74. Gunther A, Enke B, Markart P, et al. Safety and tolerability of bosentan in idiopathic pulmonary fibrosis: an open label study. Eur Respir J 2007; 29: 713-719.
75. Barst RJ, Rich S, Widlitz A, Horn EM, McLaughlin V, McFarlin J. Clinical efficacy of sitaxsentan, an endothelin-A receptor antagonist, in patients with pulmonary arterial hypertension: open-label pilot study. Chest 2002; 121: 1860-1868.
76. Galie N, Badesch D, Oudiz R, et al. Ambrisentan therapy for pulmonary arterial hypertension. J Am Coll Cardiol 2005; 46: 529-535.
77. Oudiz RJ, Badesch AB, Rubin LJ, the ARIES Study Group. ARIES-E: Long-term safety and efficacy of Ambrisentan in pulmonary arterial hypertension. Am J Respir Crit Care Med 2007; 175: A300.
78. The Task Force on Diagnosis and Treatment of Pulmonary Arterial Hypertension of the European Society of Cardiology, Guidelines on diagnosis and treatment of pulmonary arterial hypertension. Eur Heart J 2004; 25: 2243-2278.
79. Badesch DB, Abman SH, Ahearn GS, et al. Medical therapy for pulmonary arterial hypertension: ACCP evidence-based clinical practice guidelines. Chest 2004; 126: Suppl. 1, 35S-62S.
80. Liu C, Chen J. Endothelin receptor antagonists for pulmonary arterial hypertension. Cochrane Database Syst Rev 2006; Issue, 3: CD004434.