Sitaxsentan sodium for pulmonary hypertension

Drugs of Today

Volumn 44, Issue 8, 2008, Pages 585-600

  MacIntyre, Iain M ^a   Dhaun, Neeraj ^a   Goddard, Jane ^a   Webb, David J ^a  

^a UNIVERSITY OF EDINBURGH   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

AMBRISENTAN; ATRASENTAN; AVOSENTAN; BMS 207940; BOSENTAN; BSF 135252; CLAZOSENTAN; DARUSENTAN; DIURETIC AGENT; EDONENTAN; ENDOTHELIN; ENDOTHELIN RECEPTOR ANTAGONIST; ENRASENTAN; LU 125252; PROSTACYCLIN; SILDENAFIL; SITAXSENTAN; TEZOSENTAN; UNCLASSIFIED DRUG; VASODILATOR AGENT; WARFARIN;

ACUTE CORONARY SYNDROME; ACUTE HEPATITIS; AMINOTRANSFERASE BLOOD LEVEL; CONGESTIVE HEART FAILURE; DIABETIC NEPHROPATHY; DOSE RESPONSE; DRUG EFFICACY; DRUG MECHANISM; DRUG MEGADOSE; DRUG METABOLISM; DRUG TOLERABILITY; DRUG WITHDRAWAL; ESSENTIAL HYPERTENSION; HEADACHE; HEMATOCRIT; HEMOGLOBIN BLOOD LEVEL; HEPATORENAL SYNDROME; HUMAN; LIVER TOXICITY; NAUSEA; NONHUMAN; NOSE CONGESTION; OPTIMAL DRUG DOSE; PERIPHERAL EDEMA; PROSTATE CANCER; PULMONARY HYPERTENSION; REVIEW; SCLERODERMA; SIDE EFFECT; SUBARACHNOID HEMORRHAGE; TERATOGENICITY; TREATMENT INDICATION; TREATMENT OUTCOME;

ANIMALS; CLINICAL TRIALS AS TOPIC; DRUG INTERACTIONS; ENDOTHELINS; HUMANS; HYPERTENSION, PULMONARY; ISOXAZOLES; RECEPTORS, ENDOTHELIN; THIOPHENES;

EID: 56049102860     PISSN: 16993993     EISSN: 16994019     Source Type: Journal    
DOI: 10.1358/dot.2008.44.8.1239808     Document Type: Review

References (87)

1. Yanagisawa, M., Kurihara, H., Kimura, S. et al. A novel potent vasoconstrictor peptide produced by vascular endothelial cells. Nature 1988, 332(6262): 411-5.
2. Dhaun, N., Goddard, J., Webb, D.J. The endothelin system and its antagonism in chronic kidney disease. J Am Soc Nephrol 2006, 17(4): 943-55.
3. Inoue, A., Yanagisawa, M., Kimura, S., Kasuya, Y., Miyauchi, T., Goto, K., Masaki, T. The human endothelin family: Three structurally and pharmacologically distinct isopeptides predicted by three separate genes. Proc Natl Acad Sci USA 1989, 86(8): 2863-7.
4. Xu, D., Emoto, N., Giaid, A., Slaughter, C., Kaw, S., deWit, D., Yanagisawa, M. ECE-1: A membrane-bound metalloprotease that catalyzes the proteotytic activation of big endothelin-1. Cell 1994, 78(3): 473-85.
5. Kedzierski, R.M., Yanagisawa, M. Endothelin system: The double-edged sword in health and disease. Annu Rev Pharmacol Toxicol 2001, 41: 851-76.
6. Dhaun, N., Pollock, D.M., Goddard, J., Webb, D.J. Selective and mixed endothelin receptor antagonism in cardiovascular disease. Trends Pharmacol Sci 2007, 28(11): 573-9.
7. Wagner, O.F., Christ, G., Wojta, J. et al. Polar secretion of endothelin-1 by cultured endothelial cells. J Biol Chem 1992, 267(23): 16066-8.
8. Sirviö, M.L, Metsärinne, K., Saijonmaa, O., Fyhrquist, F. Tissue distribution and half-life of 1251-endothelin in the rat: Importance of pulmonary clearance. Biochem Biophys Res Commun 1990, 167(3): 1191-5.
9. Arai, H., Hori, S., Aramori, I., Ohkubo, H., Nakanishi, S. Cloning and expression of a cDNA encoding an endothelin receptor. Nature 1990, 348(6303): 730-2.
10. Sakurai, T., Yanagisawa, M., Takuwa, Y., Miyazaki, H., Kimura, S., Goto, K., Masaki, T. Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor. Nature 1990, 348(6303): 732-5.
11. Liu, S., Premont, R.T., Kontos, C.D., Huang, J., Rockey, D.C. Endothelin-1 activates endothelial cell nitric-oxide synthase via heterotrimeric G-protein beta gamma subunit signaling to protein kinase B/Akt. J Biol Chem 2003, 278(50): 49929-35.
12. McCulloch, K.M., Docherty, C.C., Morecroft, I., MacLean, M. R. EndothelinB receptor-mediated contraction in human pulmonary resistance arteries. Br J Pharmacol 1996, 119(6): 1125-30.
13. Dupuis, J., Stewart, D.J., Cemacek, P., Gosselin, G. Human pulmonary circulation is an important site for both clearance and production of endothelin-1. Circulation 1996, 94(7): 1578-84.
14. Nambi, P. Endothelin receptors in normal and diseased kidneys. Clin Exp Pharmacol Physiol 1996, 23(4): 326-30.
15. Kuc, R., Davenport, A.P. Comparison of endothelin-A and endothelin-B receptor distribution visualized by radioligand binding versus immunocytochemical localization using subtype selective antisera. J Cardiovasc Pharmacol 2004, 44(Suppl. 1): S224-6.
16. Inscho, E.W., Imig, J.D., Cook, A.K., Pollock, D.M. ETA and ETB receptors differentially modulate afferent and efferent arteriolar responses to endothelin. Br J Pharmacol 2005, 146(7): 1019-26.
17. Serneri, G.G., Modesti, P.A., Cecioni I. et al. Plasma endothelin and renal endothelin are two distinct systems involved in volume homeostasis. Am J Physiol 1995, 268(Pt. 2): H1829-37.
18. Gaine, S.P., Rubin, L.J. Primary pulmonary hypertension. Lancet 1998, 352(9129): 719-25.
19. Stewart, D.J., Levy, R.D., Cernacek, P., Langleben, D. Increased plasma endothelin-1 in pulmonary hypertension: Marker or mediator of disease? Ann Intern Med 1991, 114(6): 464-9.
20. Giaid, A., Yanagisawa, M., Langleben, D. et al. Expression of endothelin-1 in lungs of patients with pulmonary hypertension. N Engl J Med 1993, 328(24): 1732-9.
21. Dupuis, J., Cernacek, P., Tardif, J.C. et al. Reduced pulmonary clearance of endothelin-1 in pulmonary hypertension. Am Heart J 1998, 135(4): 614-20.
22. Rubens, C., Ewert, R., Halank, M., Wensel, R., Orzechowski, H.D., Schultheiss, H.P., Hoeffken, G. Big endothelin-1 and endothelin-1 plasma levels are correlated with the severity of primary pulmonary hypertension. Chest 2001, 120(5): 1562-9.
23. Soma, S., Takahashi, H., Muramatsu, M., Oka, M., Fuhi, Y. Localization and distribution of endothelin receptor subtypes in pulmonary vasculature of normal and hypoxia-exposed rats. Am J Respir Cell Mol Biol 1999, 20(4): 620-30.
24. Ivy, D., McMurtry, I.F., Yanagisawa, M. et al. Endothelin B receptor deficiency potentiates ET-1 and hypoxic pulmonary vasoconstriction. Am J Physiol Lung Cell Mol Physiol 2001, 280(5): L1040-8.
25. Ivy, D.D., McMurtry, I.F., Colvin, K. et al. Development of occlusive neointimal lesions in distal pulmonary arteries of endothelin B receptor-deficient rats: A new model of severe pulmonary arterial hypertension. Circulation 2005, 111(22): 2988-96.
26. Davie, N., Haleen, S.J., Upton, P.D. et al. ET(A) and ET(B) receptors modulate the proliferation of human pulmonary artery smooth muscle cells. Am J Respir Grit Care Med 2002, 165(3): 398-405.
27. DiCarlo, V.S., Chen, S.J., Meng, Q.C., Durand, J., Yano, M., Chen, Y.F., Oparil, S. ETA-receptor antagonist prevents and reverses chronic hypoxia-induced pulmonary hypertension in rat. Am J Physiol 1995, 269(5, Pt. 1): L690-7.
28. Chen, S.J., Chen, Y.F., Opgenorth, T.J. et al. The orally active nonpeptide endothelin A-receptor antagonist A-127722 prevents and reverses hypoxia-induced pulmonary hypertension and pulmonary vascular remodeling in Sprague-Dawley rats. J Cardiovasc Pharmacol 1997, 29(6): 713-25.
29. Chen, S.J., Chen, Y.F., Meng, Q.C., Durand, J., Dicarlo, V.S., Oparil, S. Endothelin-receptor antagonist bosentan prevents and reverses hypoxic pulmonary hypertension in rats. J Appl Physiol 1995, 79(6): 2122-31.
30. ATS Committee on Proficiency Standards for Clinical Pulmonary Function Laboratories. ATS statement: Guidelines for the six-minute walk test. Am J Respir Crit Care Med 2002, 166(1): 111-7.
31. Channick, R.N., 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(9288): 1119-23.
32. Rubin, L.J., Badesch, D.B., Barst, R.J. et al. Bosentan therapy for pulmonary arterial hypertension. N Engl J Med 2002, 346(12): 896-903.
33. McLaughlin, V.V., Sitbon, O., Badesch, D.B. et al. Survival with first-line bosentan in patients with primary pulmonary hypertension. Eur Respir J 2005, 25(2): 244-9.
34. Sandoval, J., Bauerle, O., Palomar, A., Gómez, A., Martínez-Guerra, M.L., Beltrán, M., Guerrero, M.L. Survival in primary pulmonary hypertension. Validation of a prognostic equation. Circulation 1994, 89(4): 1733-44.
35. Williamson, D.J., Wallman, L.L., Jones, R. et al. Hemodynamic effects of bosentan, an endothelin receptor antagonist, in patients with pulmonary hypertension. Circulation 2000, 102(4): 411-8.
36. Galie, N., Badesch, D., Oudiz, R. et al. Ambrisentan therapy for pulmonary arterial hypertension. J Am Coll Cardiol 2005, 46(3): 529-35.
37. Galie, N., Olschewski, H., Oudiz, R.J. et al. 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(23): 3010-9.
38. Wu, C., Chan, M.F., Stavros, F. et al. Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist. J Med Chem 1997, 40(11): 1690-7.
39. Barst, R.J., Langleben, D., Frost, A. et al. Sitaxsentan therapy for pulmonary arterial hypertension. Am J Respir Crit Care Med 2004, 169(4): 441-7.
40. Inveresk Research. Report No 175869. A phase 1 study to investigate the absorption, distribution, metabolism, and excretion of [14C]-sitaxsentan (TBC11251Na) following a single oral dose in healthy volunteers. Protocol FNL-ADME. 2004.
41. Dhaun, N., Melville, V., Kramer, W. et al. The pharmacokinetic profile of sitaxsentan, a selective endothelin receptor antagonist, in varying degrees of renal impairment. Br J Clin Pharmacol 2007, 64: 733-7.
42. Tilton, R.G., Munsch, C.L., Sherwood, S.J. et al. Attenuation of pulmonary vascular hypertension and cardiac hypertrophy with sitaxsentan sodium, an orally active ET(A) receptor antagonist. Pulm Pharmacol Ther 2000, 13(2): 87-97.
43. Givertz, M.M., Colucci, W.S., LeJemtel, T.H. et al. Acute endothelin A receptor blockade causes selective pulmonary vasodilation in patients with chronic heart failure. Circulation 2000, 101(25): 2922-7.
44. Barst, R.J., Rich, S., Widlitz, A., Horn, E.M., 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(6): 1860-8.
45. Oudiz, R.J., Barst, R.J., Hansen, J.E., Sun, X.G., Garofano, R., Wu, X., Wasserman, K. Cardiopulmonary exercise testing and six-minute walk correlations in pulmonary arterial hypertension. Am J Cardiol 2006, 97(1): 123-6.
46. Barst, R.J., 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(10): 2049-56.
47. Pulido, T., Kurzyna, M., Souza, R., Ramirez, A., Sandoval, J. Sitaxsentan 100 mg proves more effective than sitaxsentan 50 mg in patients with pulmonary arterial hypertension. Proc Am Thorac Soc 2006, 3(Abstracts Issue): Abst A417.
48. Benza, R.L., Mehta, S., Keogh, A., Lawrence, E.C., Oudiz, R.J., Barst, R.J. Sitaxsentan treatment for patients with pulmonary arterial hypertension discontinuing bosentan. J Heart Lung Transplant 2007, 26(1): 63-9.
49. Langleben, D., Hirsch, A.M., Shalit, E., Lesenko, L., Barst, R.J. 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 2004, 126(4): 1377-81.
50. Langleben, D., Hirsch, A., Shalit, E., Lesenko, L., Barst, R.J. Sustained efficacy with the selective endothelin-A receptor antagonist, sitaxsentan, after two years of therapy in patients with pulmonary arterial hypertension. 15th Annu Congr Eur Respir Soc (ERS) (Sept 17-21, Copenhagen) 2005, Abst 1334.
51. Benza, R.L., Frost, A., Grigis, R., Langleben, D., Lawrence, E.C., Naeije, R. Chronic treatment of pulmonary arterial hypertension (PAH) with sitaxsentan and bosentan. Proc Am Thorac Soc 2006, 3(Abstracts Issue): Abst A729.
52. Girgis, R.E., Keogh, A.M., Benza, R.L., Naeije, R. Incidence of abnormal liver function tests in patients with pulmonary arterial hypertension (PAH) treated for one year with sitaxsentan or bosentan. J Heart Lung Transplant 2006, 25(2): S62-3.
53. Garces, P.C., Alford, K.L., Henry, N.S., Cheeks, M., Coyne, T.C. Do liver function abnormalities with bosentan recur with sitaxsentan? 15th Annu Congr Eur Respir Soc (ERS) (Sept 17-21, Copenhagen) 2005, Abst P3624.
54. Coyne, T., Dixon, R. Warfarin management in pulmonary arterial hypertension is similar between bosentan, placebo and sitaxsentan. Chest 2005, 128(4, Suppl.): 366S.
55. Badesch, D.B., Abman, S.H., Simonneau, G., Rubin, L.J., McLaughlin, V.V. Medical therapy for pulmonary arterial hypertension: Updated ACCP evidence-based clinical practice guidelines. Chest 2007, 131(6): 1917-28.
56. Vancheeswaran, R., Magoulas, T., Efrat, G., Wheeler-Jones, C., Olsen, I., Penny, R., Black, C.M. Circulating endothelin-1 levels in systemic sclerosis subsets - A marker of fibrosis or vascular dysfunction? J Rheumatol 1994, 21(10): 1838-44.
57. Abraham, D.J., Vancheeswaran, R., Dashwood, M.R. et al. Increased levels of endothelin-1 and differential endothelin type A and B receptor expression in scleroderma-associated fibrotic lung disease. Am J Pathol 1997, 151(3): 831-41.
58. Korn, J.H., Mayes, M., Matucci Cerinic, M. et al. Digital ulcers in systemic sclerosis: Prevention by treatment with bosentan, an oral endothelin receptor antagonist. Arthritis Rheum 2004, 50(12): 3985-93.
59. Girgis, R.E., Frost, A.E., Hill, N.S. et al. Selective endothelin A receptor antagonism with sitaxsentan for pulmonary arterial hypertension associated with connective tissue disease. Ann Rheum Dis 2007, 66(11): 1467-72.
60. Schiffrin, E.L. State-of-the-art lecture. Role of endothelin-1 in hypertension. Hypertension 1999, 34(4, Pt. 2): 876-81.
61. Rossi, G.P., Colonna, S., Pavan, E. et al. Endothelin-1 and its mRNA in the wall layers of human arteries ex vivo. Circulation 1999, 99(9): 1147-55.
62. Cardillo, C., Kilcoyne, C.M., Waclawiw, M., Cannon, R.O. 3rd, Panza, J.A. Role of endothelin in the increased vascular tone of patients with essential hypertension. Hypertension 1999, 33(2): 753-8.
63. Martin, P., Ninio, D., Krum, H. Effect of endothelin blockade on basal and stimulated forearm blood flow in patients with essential hypertension. Hypertension 2002, 39(3): 821-4.
64. Krum, H., Viskoper, R.J., Lacourciere, Y., Budde, M., Charlon, V. The effect of an endothelin-receptor antagonist, bosentan, on blood pressure in patients with essential hypertension. N Engl J Med 1998, 338(12): 784-90.
65. Nakov, R., Pfarr, E., Eberle, S. Darusentan: An effective endothelinA receptor antagonist for treatment of hypertension. Am J Hypertens 2002, 15(7, Pt. 1): 583-9.
66. Battistini, B., Berthiaume, N., Kelland, N.F., Webb, DJ., Kohan, D.E. Profile of past and current clinical trials involving endothelin receptor antagonists: The novel "-sentan" class of drug. Exp Biol Med (Maywood) 2006, 231(6): 653-95.
67. Koyama, H., Tabata, T., Nishizawa, Y., Inoue, T., Morii, H., Yamaji, T. Plasma endothelin levels in patients with uraemia. Lancet 1989, 1(8645): 991-2.
68. Zoccali, C., Leonardis, D., Parlongo, S., Mallamaci, F., Postorino, M. Urinary and plasma endothelin-1 in essential hypertension and in hypertension secondary to renoparenchymal disease. Nephrol Dial Transplant 1995, 10(8): 1320-3.
69. Orisio, S., Benigni, A., Bruzzi, I. et al. Renal endothelin gene expression is increased in remnant kidney and correlates with disease progression. Kidney Int 1993, 43(2): 354-8.
70. Benigni, A. Defining the role of endothelins in renal pathophysiology on the basis of selective and unselective endothelin receptor antagonist studies. Curr Opin Nephrol Hypertens 1995, 4(4): 349-53.
71. Hocher, B., Thone-Reineke, C., Rohmeiss, P. et al. Endothelin-1 transgenic mice develop glomerulosclerosis, interstitial fibrosis, and renal cysts but not hypertension. J Clin Invest 1997, 99(6): 1380-9.
72. Ding, S.S., Qiu, C., Hess, P., Xi, J.F., Zheng, N., Clozel, M. Chronic endothelin receptor blockade prevents both early hyperfiltration and late overt diabetic nephropathy in the rat. J Cardiovasc Pharmacol 2003, 42(1): 48-54.
73. Hunley, T.E., Fogo, A., Iwasaki, S., Kon, V. Endothelin A receptor mediates functional but not structural damage in chronic cyclosporine nephrotoxicity. J Am Soc Nephrol 1995, 5(9): 1718-23.
74. Goddard, J., Johnston, N.R., Hand, M.F., Gumming, A.D., Rabelink, T.J., Rankin, A.J., Webb, D.J. Endothelin-A receptor antagonism reduces blood pressure and increases renal blood flow in hypertensive patients with chronic renal failure: A comparison of selective and combined endothelin receptor blockade. Circulation 2004, 109(9): 1186-93.
75. Motte, S., McEntee, K., Naeije, R. Endothelin receptor antagonists. Pharmacol Ther 2006, 110(3): 386-414.
76. Kobayashi, T., Miyauchi, T., Sakai, S., Kobayashi, M., Yamaguchi, I., Goto, K., Sugishita, Y. Expression of endothelin-1, ETA and ETB receptors, and ECE and distribution of endothelin-1 in failing rat heart. Am J Physiol 1999, 276(4, Pt. 2): H1197-206.
77. Pieske, B., Beyermann, B., Breu, V. et al. Functional effects of endothelin and regulation of endothelin receptors in isolated human nonfailing and failing myocardium. Circulation 1999, 99(14): 1802-9.
78. Mulder, P., Boujedaini, H., Richard, V. et al. Selective endothelin-A versus combined endothelin-A/endothelin-B receptor blockade in rat chronic heart failure. Circulation 2000, 102(5): 491-3.
79. Ohnishi, M., Wada, A., Tsutamoto, T., Fukai, D., Kinoshita, M. Comparison of the acute effects of a selective endothelin ETA and a mixed ETA/ETB receptor antagonist in heart failure. Cardiovasc Res 1998, 39(3): 617-24.
80. Mylona, P., Cleland, J.G. Update of REACH-1 and MERIT-HF clinical trials in heart failure. Cardio.net Editorial Team. Eur J Heart Fail 1999, 1(2): 197-200.
81. Lüscher, T.F., Enseleit, F., Pacher, R. et al. Hemodynamic and neurohumoral effects of selective endothelin A (ET(A)) receptor blockade in chronic heart failure: The Heart Failure ET(A) Receptor Blockade Trial (HEAT). Circulation 2002, 106(21): 2666-72.
82. Anand, I., McMurray, J., Cohn, J.N. et al. Long-term effects of darusentan on left-ventricular remodelling and clinical outcomes in the EndothelinA Receptor Antagonist Trial in Heart Failure (EARTH): Rando mised, double-blind, placebo-controlled trial. Lancet 2004, 364(9431): 347-54.
83. Bagnato, A., Rosanò, L. The endothelin axis in cancer. Int J Biochem Cell Biol 2008, 40(8): 1443-51.
84. Montironi, R., Mazzucchelli, R., Barbisan, F. et al. Immunohistochemical expression of endothelin-1 and endothelin-A and endothelin-B receptors in high-grade prostatic intraepithelial neoplasia and prostate cancer. Eur Urol 2007, 52(6): 1682-9.
85. Nelson, J.B., Chan-Tack, K., Hedican, S.P., Magnuson, S.R., Opgenorth, T.J., Bova, G.S., Simons, J.W. Endothelin-1 production and decrees ed endothelin B receptor expression in advanced prostate cancer. Cancer Res 1996, 56(4): 663-8.
86. Carducci, M.A., Padley, R.J., Breul, J. et al. Effect of endothelin-A receptor blockade with atrasentan on tumor progression in men with hormone-refractory prostate cancer: A randomized, phase II, placebocontrolled trial. J Clin Oncol 2003, 21(4): 679-89.
87. Nelson, J.B., Nabulsi, A.A., Vogelzang, N.J. et al. Suppression of prostate cancer induced bone remodeling by the endothelin receptor A antagonist atrasentan. J Urol 2003, 169(3): 1143-9.