Endothelin receptor antagonists for pulmonary arterial hypertension

Cardiovascular Therapeutics

Volumn 28, Issue 5, 2010, Pages

  Raja, Shahzad G ^a  

^a GREAT ORMOND STREET HOSPITAL   (United Kingdom)

Author keywords

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

Indexed keywords

AMBRISENTAN; BOSENTAN; CYCLOSPORIN A; ENDOTHELIN RECEPTOR ANTAGONIST; GLIBENCLAMIDE; KETOCONAZOLE; LU 208075; PROSTACYCLIN; SILDENAFIL; SIMVASTATIN; SITAXSENTAN; UNCLASSIFIED DRUG; WARFARIN;

CLINICAL TRIAL; DRUG ACTIVITY; DRUG MECHANISM; DRUG SAFETY; EXERCISE; HUMAN; LIVER TOXICITY; LUNG HEMODYNAMICS; PRIORITY JOURNAL; PULMONARY HYPERTENSION; REVIEW;

ANIMALS; ANTIHYPERTENSIVE AGENTS; BLOOD PRESSURE; DRUG INTERACTIONS; ENDOTHELINS; EVIDENCE-BASED MEDICINE; HUMANS; HYPERTENSION, PULMONARY; RECEPTORS, ENDOTHELIN; TREATMENT OUTCOME; VASODILATOR AGENTS;

EID: 77956406711     PISSN: 17555914     EISSN: 17555922     Source Type: Journal    
DOI: 10.1111/j.1755-5922.2010.00158.x     Document Type: Review

References (47)

1. Galié N, Manes A, Branzi A. The endothelin system in pulmonary arterial hypertension. Cardiovasc Res 2004 61 : 227 237. (Pubitemid 38091763)
2. Rubin LJ. Primary pulmonary hypertension. N Engl J Med 1997 336 : 111 117.
3. Galiè N, Manes A, Uguccioni L, et al. Primary pulmonary hypertension: Insights into pathogenesis from epidemiology. Chest 1998 114 : 184S 194S.
4. Hoeper MM. Definition, classification, and epidemiology of pulmonary arterial hypertension. Semin Respir Crit Care Med 2009 30 : 369 375.
5. D'Alonzo GE, Barst RJ, Ayres SM, et al. Survival in patients with primary pulmonary hypertension. Results from a national prospective registry. Ann Intern Med 1991 115 : 343 349.
6. Casserly B, Klinger JR. Ambrisentan for the treatment of pulmonary arterial hypertension. Drug Des Devel Ther 2009 2 : 265 280.
7. Matsui K, Takano Y, Yu ZX, et al. Immunohistochemical study of endothelin-1 and matrix metalloproteinases in plexogenic pulmonary arteriopathy. Pathol Res Pract 2002 198 : 403 412.
8. Jeng AY, Mulder P, Kwan AL, Battistini B. Nonpeptidic endothelin-converting enzyme inhibitors and their potential therapeutic applications. Can J Physiol Pharmacol 2002 80 : 440 449.
9. Battistini B, Berthiaume N, Kelland NF, Webb DJ, Kohn DE. Profile of past and current clinical trials involving endothelin receptor antagonists: The novel "-sentan" class of drug. Exp Biol Med (Maywood) 2006 231 : 653 695.
10. Jacobs A, Preston IR, Gomberg-Maitland M. Endothelin receptor antagonism in pulmonary arterial hypertension - a role for selective ET(A) inhibition?. Curr Med Res Opin 2006 22 : 2567 2574.
11. Takahashi T, Kanda T, Inoue M, et al. Endothelin converting enzyme inhibitor protects development of right ventricular overload and medial thickening of pulmonary arteries in rats with monocrotaline-induced pulmonary hypertension. Life Sci 1998 63 : PL137 PL143.
12. Steiner MK, Preston IR. Optimizing endothelin receptor antagonist use in the management of pulmonary arterial hypertension. Vasc Health Risk Manag 2008 4 : 943 952.
13. Raja SG, Dreyfus GD. Current status of bosentan for the treatment of pulmonary hypertension. Ann Card Anaesth 2008 11 : 6 14.
14. Kenyon KW, Nappi JM. Bosentan for the treatment of pulmonary arterial hypertension. Ann Pharmacother 2003 37 : 1055 1062.
15. Dingemanse J, van Giersbergen PL. Clinical pharmacology of bosentan: A dual endothelin receptor antagonist. Clin Pharmacokinet 2004 43 : 1089 1015.
16. Wu C, Chan MF, Stavros F, et al. Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist. J Med Chem 1997 40 : 1690 1697.
17. Widlitz AC, Barst RJ, Horn EM. Sitaxsentan: A novel endothelin-A receptor antagonist for pulmonary arterial hypertension. Expert Rev Cardiovasc Ther 2005 3 : 985 991.
18. Wu C, Decker ER, Blok N, et al. Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5- ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist. J Med Chem 2004 47 : 1969 1986.
19. Galié N, Badesch D, Oudiz R, et al. Ambrisentan therapy for pulmonary arterial hypertension. J Am Coll Cardiol 2005 46 : 529 535. (Pubitemid 41040298)
20. Cheng JW. Ambrisentan for the management of pulmonary arterial hypertension. Clin Ther 2008 30 : 825 833.
21. Barst RJ. A review of pulmonary arterial hypertension: Role of ambrisentan. Vasc Health Risk Manag 2007 3 : 11 22.
22. Barst RJ, Langleben D, Frost A, et al. STRIDE-1 Study Group. Sitaxsentan therapy for pulmonary arterial hypertension. Am J Respir Crit Care Med 2004 169 : 441 447.
23. Barst RJ, Langleben D, Badesch D, et al. STRIDE-2 Study Group. Treatment of pulmonary arterial hypertension with the selective endothelin-A receptor antagonist sitaxsentan. J Am Coll Cardiol 2006 47 : 2049 2056.
24. 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.
25. 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.
26. 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.
27. Dufton C, Gerber MJ, Yin O, Brandquist C, Ghofrani HA. No clinically relevant pharmacokinetic interaction between ambrisentan and sildenafil. Chest 2006 130 : 254S. [abstract]
28. Gerber MJ, Dufton C, Pentikis H, Zhu L, Ghofrani HA. Ambrisentan has no clinically relevant effect on the pharmacokinetics or pharmacodynamics of warfarin. Chest 2006 130 : 256S. [abstract]
29. Galié N, Badesch D, Oudiz R, et al. Ambrisentan therapy for pulmonary arterial hypertension. J Am Coll Cardiol 2005 46 : 529 535. (Pubitemid 41040298)
30. Olschewski H, Galié N, Kramer M, Rubin LJ. Ambrisentan improves exercise capacity and time to clinical worsening in patients with pulmonary arterial hypertension: Results of the ARIES-2 study. Proc Am Thorac Soc 2006 3 : A728. [abstract]
31. Oudiz R, Torres F, Frost A, et al. ARIES-1: A placebo-controlled efficacy and safety study of ambrisentan in patients with pulmonary arterial hypertension. Chest 2006 130 : 121S. [abstract]
32. Galiè N, Olschewski H, Oudiz RJ, et al. Ambrisentan in Pulmonary Arterial Hypertension, Randomized, Double-Blind, Placebo-Controlled, Multicenter, Efficacy Studies (ARIES) Group. Ambrisentan for the treatment of pulmonary arterial hypertension: Results of the ambrisentan in pulmonary arterial hypertension, randomized, double-blind, placebo-controlled, multicenter, efficacy (ARIES) study 1 and 2. Circulation 2008 117 : 3010 3019.
33. Rubin LJ, Badesch DB, Barst RJ, Galiè N, Black CM, Keogh A. Bosentan therapy for pulmonary arterial hypertension. N Eng J Med 2002 346 : 896 903. (Pubitemid 34984638)
34. 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. (Pubitemid 39232254)
35. Galiè N, Beghetti M, Gatzoulis MA, et al. Bosentan Randomized Trial of Endothelin Antagonist Therapy-5 (BREATHE-5) Investigators. Bosentan therapy in patients with Eisenmenger syndrome: A multicenter, double-blind, randomized, placebo-controlled study. Circulation 2006 114 : 48 54.
36. Channick RN, Simonneau G, Sitbon O, Robbins IM, Frost A, Tapson VF. Effects of the dual endothelin-receptor antagonist bosentan in patients with pulmonary hypertension: A randomised placebo-controlled study. Lancet 2001 358 : 1119 1123. (Pubitemid 32971843)
37. Galiè N, Rubin L, Hoeper 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 : 2093 2100.
38. European Medicines Agency. EPARs for authorised medicinal products for human use: Thelin. European Public Assessment Report. http://www.emea.europa.eu/ humandocs/PDFs/EPAR/thelin/H-679-en6.pdf (Accessed December 22 2009).
39. Wilkins MR, Paul GA, Strange JW, et al. Sildenafil versus Endothelin Receptor Antagonist for Pulmonary Hypertension (SERAPH) study. Am J Respir Crit Care Med 2005 171 : 1292 1297.
40. Liu C, Chen J, Gao Y, Deng B, Liu K. Endothelin receptor antagonists for pulmonary arterial hypertension. Cochrane Database Syst Rev 2009. doi :.
41. Benza RL, Frost A, Girgis R, Langleben D, Lawrence EC, Naeije R. Chronic treatment of pulmonary arterial hypertension (PAH) with sitaxentan and bosentan. Proc Am Thorac Soc 2006 3 : A729. [abstract]
42. Opitz CF, Ewert R, Kirch W, Pittrow D. Inhibition of endothelin receptors in the treatment of pulmonary arterial hypertension: Does selectivity matter?. Eur Heart J 2008 29 : 1936 1948.
43. 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 : 223 231.
44. Fouassier L, Kinnman N, Lefèvre G, et al. Contribution of mrp2 in alterations of canalicular bile formation by the endothelin antagonist bosentan. J Hepatol 2002 37 : 184 191.
45. Brouwer KR, Wille KR, Gorczynski RJ. Ambrisentan, darusentan, bosentan, and sitaxsentan: Differences in inhibition of hepatobilliary transporters in two species. Drug Metab Rev 2007 39 (suppl 1 388. [abstract]
46. McGoon MD, Frost AE, Oudiz RJ, et al. Ambrisentan therapy in patients with pulmonary arterial hypertension who discontinued bosentan or sitaxsentan due to liver function test abnormalities. Chest 2009 135 : 122 129.
47. Spence S, Anderson C, Cukierski M, Patrick D. Teratogenic effects of the endothelin receptor antagonist L-753,037 in the rat. Reprod Toxicol 1999 13 : 15 29.