Optimizing endothelin receptor antagonist use in the management of pulmonary arterial hypertension

Vascular Health and Risk Management

Volumn 4, Issue 5, 2008, Pages 943-952

  Steiner, M Kathryn ^a   Preston, Iona R ^b  

^a MASSACHUSETTS GENERAL HOSPITAL   (United States)

^b TUFTS MEDICAL CENTER   (United States)

Author keywords

Ambrisentan; Bosentan; Endothelin receptor antagonists; Pulmonary arterial hypertension; Sitaxsentan

Indexed keywords

AMBRISENTAN; ANTIRETROVIRUS AGENT; BERAPROST; BOSENTAN; CYCLOSPORIN A; ENDOTHELIN RECEPTOR ANTAGONIST; GLIBENCLAMIDE; ILOPROST; LETAIRIS; PLACEBO; PROSTACYCLIN; SILDENAFIL; SITAXSENTAN; UNCLASSIFIED DRUG; WARFARIN;

ABSENCE OF SIDE EFFECTS; AMINOTRANSFERASE BLOOD LEVEL; CLINICAL TRIAL; COMBINATION CHEMOTHERAPY; DIZZINESS; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG DOSE COMPARISON; DRUG DOSE INCREASE; DRUG DOSE REDUCTION; DRUG DOSE TITRATION; DRUG EFFICACY; DRUG EXCRETION; DRUG FATALITY; DRUG HALF LIFE; DRUG INDUCED HEADACHE; DRUG MECHANISM; DRUG MEGADOSE; DRUG METABOLISM; DRUG PROTEIN BINDING; DRUG RESPONSE; DRUG SAFETY; DRUG STRUCTURE; DRUG SUBSTITUTION; DRUG TOLERABILITY; DRUG WITHDRAWAL; HUMAN; LIVER FUNCTION; LIVER TOXICITY; LOW DRUG DOSE; LUNG HEMODYNAMICS; MONOTHERAPY; NAUSEA; NONHUMAN; NOSE CONGESTION; PATIENT SATISFACTION; PERIPHERAL EDEMA; PULMONARY HYPERTENSION; QUALITY OF LIFE; RECOMMENDED DRUG DOSE; REVIEW; SIDE EFFECT; SURVIVAL RATE; VASCULAR RESISTANCE;

ANIMALS; ANTIHYPERTENSIVE AGENTS; DRUG THERAPY, COMBINATION; HUMANS; HYPERTENSION, PULMONARY; ISOXAZOLES; PATIENT COMPLIANCE; PATIENT SATISFACTION; PHENYLPROPIONATES; PYRIDAZINES; QUALITY OF LIFE; RECEPTORS, ENDOTHELIN; SULFONAMIDES; THIOPHENES; TREATMENT OUTCOME;

EID: 56849118453     PISSN: 11766344     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (68)

1. Arai H, Hori S, Aramori I, et al. 1990. Cloning and expression of a cDNA encoding an endothelin receptor. Nature, 348:730-2.
2. Barst RJ, Ivy D, Dingemanse J, et al. 2003. Pharmacokinetics, safety, and efficacy of bosentan in pediatric patients with pulmonaiy arterial hypertension. Clin Pharmacol Ther, 73:372-82.
3. Barst RJ, Langleben D, Badesch D, et al. 2006. Treatment of pulmonary arterial hypertension with the selective endothelin-A receptor antagonist sitaxsentan. [see comment]. J Am Coll Cardiol, 47:2049-56.
4. Barst RJ, Langleben D, Frost A, et al. 2000. Sitaxsentan therapy for pulmonary arterial hypertension. Am J Resp Crit Care Med, 169:441-7.
5. Barst RJ, Rich S, Widlitz A, et al. 2002. Clinical efficacy of sitaxsentan, an endothelin-A receptor antagonist, in patients with pulmonary arterial hypertension: open-label pilot study. Chest, 121:1860-8.
6. Battistini B, Berthiaume N, Kelland NF, et al. 2006. Profile of past and current clinical trials involving endothelin receptor antagonists: the novel "sentan" class of drug. Exp Biol Med (Maywood), 231:653-95.
7. Benza RL, Frost A, Girgis RE, et al. 2006. Chronic treatment of pulmonary artenal hypertension with sitaxsentan and bosentan [abstract]. Proc Am Thorac Soc, 3:A729.
8. Benza RL, Mehta S, Keogh A, et al. 2007. Sitaxsentan treatment for patients with pulmonary arterial hypertension discontinuing bosentan. J Heart Lung Transplant, 26:63-9.
9. Black SM, Mata-Greenwood E, Dettman RW, et al. 2003. Emergence of smooth muscle cell endothelin B-mediated vasoconstriction in lambs with experimental congenital heart disease and increased pulmonary blood flow. Circulation, 108:1646-54.
10. Bonderman D, Nowotny R, Skoro-Sajer N, et al. 2005. Bosentan therapy for inoperable chronic thromboembolic pulmonary hypertension. Chest, 128:2599-603.
11. Channick RN, Simonneau G, Sitbon O, et al. 2001. Effects of the dual endothelin-receptor antagonist bosentan in patients with pulmonary hypertension: a randomised placebo-controlled study. Lancet, 358:1119-23.
12. Davie N, Haleen SJ, Upton PD, et al. 2002a. ET(A) and ET(B) receptors modulate the proliferation of human pulmonary artery smooth muscle cells. Am J Respir Crit Care Med, 165:398-405.
13. Davie N, Haleen SJ, Upton PD, et al. 2002b. ET(A) and ET(B) receptors modulate the proliferation of human pulmonary artery smooth muscle cells. Am J Resp Crit Care Med, 165:398-405.
14. de Nucci G, Thomas R, D'Orleans-Juste P, et al. 1988. Pressor effects of circulating endothelin are limited by its removal in the pulmonary circulation and by the release of prostacyclin and endothelium-derived relaxing factor. Proc Natl Acad Sci USA, 85:9797-800.
15. Dingemanse J, Bodin F, Weidekamm E, et al. 2002a. Influence of food intake and formulation on the pharmacokinetics and metabolism of bosentan, a dual endothelin receptor antagonist. J Clin Pharmacol, 42:283-9.
16. Dingemanse J, Bodin F, Weidekamm E, et al. 2002b. Influence of food intake and formulation on the pharmacokinetics and metabolism of bosentan, a dual endothelin receptor antagonist. J Clin Pharmacol, 42:283-9.
17. Dupuis J, Goresky CA, Fournier A. 1996a. Pulmonary clearance of circulating endothelin-1 in dogs in vivo: exclusive role of ETB receptors. J Appl Physiol, 81:1510-5.
18. Dupuis J, Stewart DJ, Cernacek P, et al. 1996b. Human pulmonary circulation is an important site for both clearance and production of endothelin-1. Circulation, 94:1578-84.
19. Evans AM, Cobban HJ, Nixon GF. 1999. ET(A) receptors are the primary mediators of myofilament calcium sensitization induced by ET-1 in rat pulmonary artery smooth muscle: a tyrosine kinase independent pathway. Br J Pharmacol, 127:153-60.
20. Galie N, Badesch D, Oudiz R, et al. 2005. Ambrisentan therapy for pulmonary arterial hypertension. J Am Coll Cardiol, 46:529-35.
21. Galie N, Beghetti M, Gatzoulis MA, et al. 2006. Bosentan therapy in patients with Eisenmenger syndrome: a multicenter, double-blind, randomized, placebo-controlled study. Circulation, 114:48-54.
22. Galie N, Hinderliter AL, Torbicki A, et al. 2003. Effects of the oral endothelin-receptor antagonist bosentan on echocardiographic and doppler measures in patients with pulmonary arterial hypertension. J Am Coll Cardiol, 41:1380-6.
23. Giaid A, Yanagisawa M, Langleben D, et al. 1993. Expression of endothelin-1 in the lungs of patients with pulmonary hypertension. N Engl J Med, 328:1732-9.
24. Girgis RE, Frost AE, Hill NS, et al. 2007. Selective endothelinA receptor antagonism with sitaxsentan for pulmonary arterial hypertension associated with connective tissue disease. Ann Rheum Dis, 66:1467-72.
25. Hoeper MM, Kramm T, Wilkens H, et al. 2005. Bosentan therapy for inoperable chronic thromboembolic pulmonary hypertension. Chest, 128:2363-67.
26. Hoeper MM, Leuchte H, Halank M, et al. 2006. Combining inhaled iloprost with bosentan in patients with idiopathic pulmonary arterial hypertension. Eur Respir J, 28:691-94.
27. Hoeper MM, Taha N, Bekjarova A, et al. 2003. Bosentan treatment in patients with primary pulmonary hypertension receiving nonparenteral prostanoids. Eur Respir J, 22:330-4.
28. Humbert M, Barst RJ, Robbins IM, et al. 2004. Combination of bosentan with epoprostenol in pulmonary arterial hypertension: BREATHE-2. Eur Respir J, 24:353-9.
29. Humbert M, Morrell NW, Archer SL, et al. 2004. Cellular and molecular pathobiology of pulmonary arterial hypertension. J Am Coll Cardiol, 43:13S-24S.
30. Humbert M, Segal ES, Kiely DG, et al. 2007. Results of European post-marketing surveillance of bosentan in pulmonary hypertension. Eur Respir J, 30:338-44.
31. Ivy DD, Doran A, Claussen L, et al. 2004. Weaning and discontinuation of epoprostenol in children with idiopathic pulmonary arterial hypertension receiving concomitant bosentan. Am J Cardiol, 93:943-6.
32. Jankov RP, Kantores C, Belcastro R, et al. 2006. Endothelin-1 inhibits apoptosis of pulmonary arterial smooth muscle in the neonatal rat. Pediatr Res, 60:245-51.
33. Jasmin JF, Lucas M, Cernacek P, et al. 2001. Effectiveness of a nonselective ET(A/B) and a selective ET(A) antagonist in rats with monocrotaline-induced pulmonary hypertension. Circulation, 103:314-9.
34. Kim NH, Channick RN, and Rubin LJ 2003. Successful withdrawal of long-term epoprostenol therapy for pulmonary arterial hypertension. Chest, 124:1612-5.
35. Langleben D, Dupuis J, Langleben I, et al. 2006. Etiology-specific endothelin-1 clearance in human precapillary pulmonary hypertension. Chest, 129:689-95.
36. Langleben D, Hirsch AM, Shalit E, et al. 2004. Sustained symptomatic, functional, and hemodynamic benefit with the selective endothelin. A receptor antagonist, sitaxsentan, in patients with pulmonary arterial hypertension: a 1-year follow-up study. Chest, 126:1377-81.
37. McCulloch KM, Docherty CC, Morecroft I, et al. 1996. EndothelinB receptor-mediated contraction in human pulmonary resistance arteries. Br J Pharmacol, 119:1125-30.
38. McLaughlin VV, Oudiz RJ, Frost A, et al. 2006. Randomized study of adding inhaled iloprost to existing bosentan in pulmonary arterial hypertension. Am J Respir Crit Care Med, 174:1257-63.
39. McLaughlin VV, Sitbon O, Badesch DB, et al. 2005. Survival with first-line bosentan in patients with primary pulmonary hypertension. [erratum Eur Respir J, 2005 25:942]. Eur Respir J, 25:244-9.
40. Mathai SC, Girgis RE, Fisher MR, et al. 2007. Addition of sildenafil to bosentan monotherapy in pulmonary arterial hypertension. Eur Respir J, 29:469-75.
41. Michelakis ED. 2006. Spatio-temporal diversity of apoptosis within the vascular wall in pulmonary arterial hypertension: heterogeneous BMP signaling may have therapeutic implications. Circ Res, 98:72-5.
42. Murphey L, Hood E 2003. Bosentan and warfarin interaction. Ann Pharmacother, 37:1028-31.
43. Olschewski H, Galie N, Kramer M, et al. 2006. Ambrisentan improves exercise capacity and time to clinical worsening in patients with pulmonary arterial hypertension: results of the ARIES-2 study [abstract]. Proc Am Thorac Soc, 3:A278.
44. Oudiz R, Torres F, Frost A, et al. 2006. ARIES-1: A placebo controlled, efficacy and safety study of ambrisentan in patients with pulmonary arterial hypertension. Chest, 130:121S.
45. Oudiz RJ, Barst RJ, Hansen JE, et al. 2006. Cardiopulmonary exercise testing and six-minute walk correlations in pulmonary arterial hypertension. Am J Cardiol, 97:123-6.
46. Paul GA, Gibbs JS, Boobis AR, et al. 2005. Bosentan decreases the plasma concentration of sildenafil when coprescribed in pulmonary hypertension. Br J Clin Pharmacol, 60:107-12.
47. Pulido T, Kurzyna M, Souza R, et al. 2006. Sitaxsentan 100 mg proves more effective than sitaxsentan 50 mg patients with pulmonary arterial hypertension [abstract]. Proc Am Thorac Soc, 3:A417.
48. Rubin JL, Simonneau G, Hoeper MM, et al. 2007. Bosentan improves hemodynamics in patients receiving backgroundsildenafil treatment: results from EARLY, a randomized, double-blind, placebo-controlled study in patients with mildly symptomatic pulmonary arterial hypertension [abstract]. Chest, 132:487S.
49. Rubin LJ, Badesch DB, Barst RJ, et al. 2002. Bosentan therapy for pulmonary arterial hypertension. [erratum N Engl J Med, 2002 346:1258]. N Engl J Med, 346:896-903.
50. Sakurai T, Yanagisawa M, Takuwa Y, et al. 1990. Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor. Nature, 348:732-5.
51. Sato K, Oka M, Hasunuma K, et al. 1995. Effects of separate and combined ETA and ETB blockade on ET-1-induced constriction in perfused rat lungs. Am J Physiol, 269:L668-672.
52. Shichiri M, Kato H, Maninto F, et al. 1997. Endothelin-1 as an autocrine/ paracrine apoptosis survival factor for endothelial cells. Hypertension, 30:1198-203.
53. Sitbon O, Badesch DB, Channick RN, et al. 2003. Effects of the dual endothelin receptor antagonist bosentan in patients with pulmonary arterial hypertension: a 1-year follow-up study. Chest, 124:247-54.
54. Sitbon O, Gressin V, Speich R, et al. 2004. Bosentan for the treatment of human immunodeficiency virus-associated pulmonary arterial hypertension. Am J Respir Crit Care Med, 170:1212-7.
55. Sitbon O, McLaughlin VV, Badesch DB, et al. 2005. 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, 60:1025-30.
56. Spence S, Anderson C, Cukierski M, et al. 1999. Teratogenic effects of the endothelin receptor antagonist L-753,037 in the rat. [erratum Reprod Toxicol, 1999 13:237]. Reprod Toxicol, 13:15-29.
57. Steiner MK, Preston IR, Klinger JR, et al. 2006. Conversion to bosentan from prostacyclin inftision therapy in pulmonary arterial hypertension: a pilot study. Chest, 130:1471-80.
58. Suleman N, Frost AE. 2004. Transition from epoprostenol and treprostinil to the oral endothelin receptor antagonist bosentan in patients with pulmonary hypertension. Chest, 126:808-15.
59. Treiber A, Schneiter R, Hausler S, et al. 2007. Bosentan is a substrate of human OATP1B1 and OATP1B3: inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil. Drug Metab Dispos, 35:1400-7.
60. van Giersbergen PL, Halabi A, Dingemanse J. 2002a. Single- and multiple-dose pharmacokineties of bosentan and its interaction with ketoconazole. Br J Clin Pharmacol, 53:589-95.
61. van Giersbergen PL, Treiber A, Clozel M, et al. 2002b. In vivo and in vitro studies exploring the pharmacokinetic interaction between bosentan, a dual endothelin receptor antagonist, and glyburide. Clin Pharmacol Ther, 71:253-62.
62. Voelkel NF, Cool C, Lee SD, et al. 1998. Primary pulmonary hypertension between inflammation and cancer. Chest, 114:225S-30S.
63. Weber C, Schmitt R, Birnboeck H, et al. 1996a. Pharmacokinetics and pharmacodynamics of the endothelin-receptor antagonist bosentan in healthy human subjects. Clin Pharmacol Ther, 60:124-37.
64. Weber C, Schmitt R, Birnboeck H, et al. 1996b. Pharmacokinetics and pharmacodynamics of the endothelin-receptor antagonist bosentan in healthy human subjects. Clin Pharmacol Ther, 60:124-37.
65. Widlitz AC, Barst RJ, Horn EM. 2005. Sitaxsentan: a novel endothelin. A receptor antagonist for pulmonary arterial hypertension. Expert Rev Cardiovasc Ther, 3:985-91.
66. Williamson DJ, Wallman LL, Jones R, et al. 2000. Hemodynamic effects of bosentan, an endothelin receptor antagonist, in patients with pulmonary hypertension. Circulation, 102:411-8.
67. Wu C, Decker ER, Blok N, et al. 2004a. Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl) thio phene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist. J Med Chem, 47:1969-86.
68. Wu C, Decker ER, Blok N, et al. 2004b. Discovery, modeling, and human pharmacokinetics of