171
Views
54
CrossRef citations to date
0
Altmetric
Miscellaneous

Bosentan: a dual endothelin receptor antagonist

&
Pages 991-1002 | Published online: 24 Feb 2005

Bibliography

  • HAYNES WG, WEBB DJ: The endothelin family of peptides: local hormones with diverse roles in health and disease? Clin. Sci. (1993) 84:485–500.
  • LEVIN ER: Endothelins. N Engl. I Med. (1995) 333:356–363.
  • ••Comprehensive review of endothelins and their role in health and disease.
  • HIRATA Y, EMORI T, EGUCHI S et al:Endothelin receptor subtype B mediates synthesis of nitric oxide by cultured bovine endothelial cells. Clin. Invest. (1993) 91:1367–1373.
  • FILEP JG, HERMAN F, BATTISTINI B, CHABRIER P-E, BRAQUET P, SIROIS P: Antiaggretory and hypotensive effects of endothelin-1 in beagle dogs: role for prostacyclin. Cardiovasc. Pharrnacol. (1991) 17\(Suppl. 7):S216–S218.
  • CANNAN CR, BURNETT Jr JC, LERMAN A: Enhanced coronary vasoconstriction to endothelin-B receptor activation in experimental congestive heart failure. Circulation (1996) 93:646–651.
  • CARDILLO C, KILCOYNE CM, WACLAWIW M, CANNON III RO, PANZA JA: Role of endothelin in the increased vascular tone of patients with essential hypertension. Hypertension (1999) 33:753–758.
  • ABRAHAM DJ, VANCHEESWARAN R, DASHWOOD MR 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) 151:831–841.
  • •A study on the distribution and expression levels of ET and ET receptors in sderoderma-associated lung disease.
  • BAUER M, WILKENS H, LANGER F, SCHNEIDER SO, LAUSBERG H, SCHAFERS H-J: Selective upregulation of endothelin B receptor gene expression in severe pulmonary hypertension. Circulation (2002) 105:1034–1036.
  • LAUTH M, BERGER M-M, CATTARUZZA M, HECKER M: Elevated perfusion pressure upregulates endothelin-1 and endothelin B receptor expression in the rabbit carotid artery. Hypertension (2000) 35:648–654.
  • YOKOYAMA Y, BAVEJA R, SONIN N, NAKANISHI K, ZHANG JX, CLEMENS MG: Altered endothelin receptor subtype expression in hepatic injury after ischemia/ reperfusion. Shock (2000) 13:72–78.
  • FUKURODA T, FUJIKAWA T, OZAKI S, ISHIKAWA K, YANO M, NISHIKIBE M: Clearance of circulating endothelin-1 by ETB receptors in rats. Biochem. Biophys. Res. Commun. (1994) 199:1461–1465.
  • ITO H, HIRATA Y, HIROE M et al: Endothelin-1 induces hypertrophy with enhanced expression of muscle-specific genes in cultured neonatal rat cardiomyocytes. Circulation (1991) 69:209–215.
  • PEACOCK AJ, DAWES KE, SHOCK A, GRAY AJ, REEVES JT, LAURENT GJ: Endothelin-1 and endothelin-3 induce chemotaxis and replication of pulmonary artery fibroblasts. Am. f Respic Cell Mol Biol. (1992) 7:492–499.
  • PIACENTINI L, GRAY M, HONBO NY, CHENTOUFI J, BERGMAN M, KARLINER JS: Endothelin-1 stimulates cardiac fibroblast proliferation through activation of protein kinase Cf Mol Cell Cardiol (2000) 32:565–576.
  • DAVIE N, HALEEN SJ, UPTON PD et al: ETA and ETB receptors modulate the proliferation of human pulmonary artery smooth muscle cells. Am. f Respir: Crit. Care Med. (2002) 165:398–405.
  • TEDER P, NOBLE PW: A cytokine reborn? Endothelin-1 in pulmonary inflammation and fibrosis. Am. J. Respir. Cell Ma Biol. (2000) 23:7–10.
  • ROSSI GP, ALBERTIN G, NERI G et al: Endothelin-1 stimulates steroid secretion of human adrenocortical cells ex vivo via both ETA and ETB receptor subtypes. I Clin. Endocrinol Metab. (1997) 82:3445–3449.
  • SOTSCH G, BERTEL 0, RICKENBACHER P et al.: Regulation of aldosterone secretion in patients with chronic congestive heart failure by endothelins. Am. Cardiol (2000) 85:973–976.
  • GIAID A, YANAGISAWA M, LANGLEBEN D et al: Expression of endothelin-1 in the lungs of patients with pulmonary hypertension. N Engl. I Med. (1993) 328:1732–1739.
  • •Presents histological evidence for ET-1 in pulmonary hypertension.
  • VEYSSIER-BELOT C, CACOUB P: Role of endothelial and smooth muscle cells in the physiopathology and treatment management of pulmonary hypertension. Cardiovasc. Res. (1999) 44:274–282.
  • •Review of the molecular factors involved in the pathophysiology of pulmonary hypertension and implications for its management.
  • MIYAUCHI T, YORIKANE R, SAKAI S et al.: Contribution of endogenous endothelin-1 to the progression of cardiopulmonary alterations in rats with monocrotaline-induced pulmonary hypertension. Circ. Res. (1993) 73:887–897.
  • STELZNER TJ, O'BRIEN RE YANAGISAWA M et al.: Increased lung endothelin-1 production in rats with idiopathic pulmonary hypertension. Am. Physiol (1992) 262:L614–L620.
  • CACOUB P, DORENT R, NATAF P et al: Endothelin-1 in the lungs of patients with pulmonary hypertension. Cardiovasc. Res. (1997) 33:196–200.
  • YOSHIBAYASHI M, NISHIOKA K, NAKAO K et al.: Plasma endothelin concentrations in patients with pulmonary hypertension associated with congenital heart defects: evidence for increased production of endothelin in pulmonary circulation. Circulation (1991) 84:2280–2285.
  • RUBIN U. ACCP consensus statement: primary pulmonary hypertension. Chest (1993) 104:236–250.
  • ABENHAIM L, MORIDE Y, BRENOT F et al.: Appetite-suppressant drugs and the risk of primary pulmonary hypertension. N Engl. Med. (1996) 335:609–616.
  • GAINE SP, RUBIN LJ: Primary pulmonary hypertension. Lancet (1998) 352:719–725.
  • •Comprehensive review of primary pulmonary hypertension.
  • RUBIN LJ: Primary pulmonary hypertension. N Engl. I Med. (1997) 336:111–117.
  • •Overview of the current understanding of primary pulmonary hypertension.
  • RICH S, DANTZKER DR, AYERS SM et al: Primary pulmonary hypertension: a national prospective study. Ann. Intern. Med. (1987) 107:216–223.
  • 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.
  • •Large evaluation of the survival rates and factors associated with survival in patients with primary pulmonary hypertension.
  • OAKLEY CW: Primary pulmonary hypertension: case series from the United Kingdom. Chest (1994) 105(Suppl.):295-32S.
  • KOH ET, LEE P, GLADMAN DD, ABU-SHAKRA M. Pulmonary hypertension in systemic sclerosis: an analysis of 17 patients. Br. Rheumatol (1996) 35:989–993.
  • STUPI AM, STEEN VD, OWENS GR, BARNES EL, RODNAN GP, MEDSGER Jr TA: Pulmonary hypertension in the CREST syndrome variant of systemic sclerosis. Arthritic Rheum. (1986) 29:515–524.
  • SHAPIRO SM, OUDIZ RJ, CAO T et al:Primary pulmonary hypertension: improved long-term effects and survival with continuous intravenous epoprostenol infusion. I Am. Coll. Cardiol (1997) 30:343–349.
  • THE INTERNATIONAL PPH CONSORTIUM, LANE KB, MACHADO RD et al.: Heterozygous germline mutations in BMPR2, encoding a TGF-B receptor, cause familial primary pulmonary hypertension. Nat. Genet. (2000) 26:81–84.
  • THOMSON JR, MACHADO RD, PAUCIULO MW et al.: Sporadic primary pulmonary hypertension is associated with germline mutations of the gene encoding BMPR-II, a receptor member of the TGF-B family. Med. Genet. (2000) 37:741–745.
  • RICH S, KAUFMANN E, LEVY PS: Theeffect of high doses of calcium-channel blockers on survival in primary pulmonary hypertension. N Engl. I Med. (1992) 327:76–81.
  • SITBON 0, HUMBERT M, JAGOT J-Let al.: Inhaled nitric oxide as a screening agent for safely identifying responders to oral calcium-channel blockers in primary pulmonary hypertension. Ear: Respic (1998) 12:265–270.
  • RICH S, BRUNDAGE B: High-dose calcium channel-blocking therapy for primary pulmonary hypertension: evidence for long-term reduction in pulmonary arterial pressure and regression of right ventricular hypertrophy. Circulation (1987) 76:135–141.
  • BADESCH DB, TAPSON VF, MCGOON MD et al.: Continuous intravenous epoprostenol for pulmonary hypertension due to the scleroderma spectrum of disease: a randomized, controlled trial. Ann. Intern. Med. (2000) 132:425–434.
  • BARST RJ, RUBIN LJ, LONG WA et al: A comparison of continuous intravenous epoprostenol (prostacyclin) with conventional therapy for primary pulmonary hypertension. N Engl. I Med. (1996) 334:296–301.
  • BARST RJ, RUBIN LJ, MCGOON MD et al.: Survival in primary pulmonary hypertension with long-term continuous intravenous prostacyclin. Ann. Intern. Med. (1994) 121:409–415.
  • WANSTALL JC, JEFFERY TK: Recognition and management of pulmonary hypertension. Drugs (1998) 56:989–1007.
  • GARDINER SM, KEMP PA, MARCH JE, BENNETT T: Effects of bosentan (Ro 47-0203), an ETA-, ETB-receptor antagonist, on regional haemodynamic responses to endothelins in conscious rats. Br. Pharmacol (1994) 112:823–830.
  • CARRATU P, SCURI M, STYBLO JL, WANNER A, GLASSBERG MK: ET-1 induces mitogenesis in ovine airway smooth muscle cells via ETA and ETBreceptors. Am. Physiol. (1997) 272:L1021–L1024.
  • KATWA LC, GUARDA E, WEBER KT: Endothelin receptors in cultured rat cardiac fibroblasts. Cardiovasc. Res. (1993) 27:2125–2129.
  • MCCULLOCH KM, DOCHERTY CC, MORECROFT I, MACLEAN MR: Endotheling receptor-mediated contraction in human pulmonary resistance arteries. Br..! Pharmacol (1996) 119:1125–1130.
  • CLOZEL M, BREU V, GRAY GA et al.: Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. Pharmacol Exp. The]: (1994) 270:228–235.
  • ••Original pharmacological characterisationof bosentan.
  • ROUX S, BREU V, ERTEL SI, CLOZEL M: Endothelin antagonism with bosentan: a review of potential applications. J. MM. Med. (1999) 77:364–376.
  • CHAMPION HC, ESTRADA LS, ESTRADA LN, FILEP JG, KADOWITZ PJ: Analysis of effects of bosentan (Ro 47-0203), a nonpeptide endothelin ETA/ETB receptor antagonist, in the hind-limb vascular bed of the cat. Can. Physiol Pharmacol (1998) 76:141–147.
  • DOMKOWSKI PW, COCKERHAM JT, KOT PA, MYERS JL, HOPKINS RA: Characterization of the pulmonary arterial response to endothelin-1 and bosentan in neonatal pigs. Ann. Thome. Surg. (2000) 70:1522–1530.
  • MARTIN C, HELD HD, UHLIG S: Differential effects of the mixed ET(A)/ ET(B)-receptor antagonist bosentan on endothelin-induced bronchoconstriction, vasoconstriction and prostacyclin release. Naunyn Schmiedebergs Arch. Pharmacol (2000) 362:128–136.
  • ROSSI GP, SACCHETTO A, RIZZONI D et al.: Blockade of angiotensin II Type 1 receptor and not of endothelin receptor prevents hypertension and cardiovascular disease in transgenic (mREN2)27 rats via adrenocortical steroid-independent mechanisms. Arteriosc/er. Thromb. V3SC. Bid (2000) 20:949–956.
  • HESS P, CLOZEL M, CLOZEL J-P: Telemetry monitoring of pulmonary arterial pressure in freely moving rats.' Appl. Physiol (1996) 81:1027–1032.
  • CHEN S-J, CHEN Y-F, MENG QC, DURAND J, DICARLO VS, OPARIL S: Endothelin-receptor antagonist bosentan prevents and reverses hypoxic pulmonary hypertension in rats. Appl Physiol (1995) 79:2122–2131.
  • EDDAHIBI S, RAFFESTIN B, CLOZEL M, LEVAME M, ADNOT S: Protection from pulmonary hypertension with an orally active endothelin receptor antagonist in hypoxic rats. Am. Physiol (1995) 268:H828–H835.
  • HOLM P, LISKA J, CLOZEL M, FRANCO-CERECEDA A: The endothelin antagonist bosentan: hemodynamic effects during normwda and hypoxic pulmonary hypertension in pigs.' Thome. Cardiovasc. Surg. (1996) 112:890–897.
  • WANECEK M, OLDNER A, RUDEHILL A, SOLLEVI A, ALVING K, WEITZBERG E: Cardiopulmonary dysfunction during porcine endotoxin shock is effectively counteracted by the endothelin receptor antagonist bosentan. Shock (1997) 7:364–370.
  • KIM H, YUNG GL, MARSH JJ et al: Endothelin mediates pulmonary vascular remodelling in a canine model of chronic embolic pulmonary hypertension. Ear. Respir. (2000) 15:640–648.
  • PARK S-H, SALEH D, GIAID A, MICHEL RP: Increased endothelin-1 in bleomycin-induced pulmonary fibrosis and the effect of an endothelin receptor antagonist. Am. Resp. Grit. Care Med (1997) 156:600–608.
  • ••Study of the role of ET and bosentan in arodent model of pulmonary fibrosis.
  • MULDER P, RICHARD V, DERUMEAUX G et al.: Role of endogenous endothelin in chronic heart failure: effect of long-term treatment with an endothelin antagonist on survival, hemodynamics, and cardiac remodeling. Circulation (1997) 96:1976–1982.
  • MISHIMA T, TANIMURA M, SUZUKI G et al.: Effects of long-term therapy with bosentan on the progression of left ventricular dysfunction and remodeling in dogs with heart failure. Am. Coll. Cardiol (2000) 35:222–229.
  • HERBERT KJ, HICKEY MJ, LEPORE DA, KNIGHT KR, MORRISON WA, STEWART AG: Effects of the endothelin receptor antagonist bosentan on ischaemia/ reperfusion injury in rat skeletal muscle. Ear: Pharmacol (2001) 424:59–67.
  • FILEP JG, FOURNIER A, FOLDES-FILEP È: Acute pro-inflammatory actions of endothelin-1 in the guinea-pig lung: involvement of ETA and ETB receptors. Br. Pharmacol (1995) 115:227–236.
  • GUIMARAES CL, DA SILVA S, COUTURE R, RAE GA: Mixed endothelin ET(A) and ET(B) antagonist bosentan inhibits oleic acid-induced lung plasma extravasation in mouse.' Cardiovasc. Pharmacol (2000) 36(5, Suppl. 1):S371–S373.
  • BRANDLI P, LOFFLER B-M, BREU V, OSTERWALDER R, MAIRE J-P, CLOZEL M: Role of endothelin in mediating neurogenic plasma extravasation in rat dura mater. Pain (1995) 64:315–322.
  • KIOWSKI W, SOTSCH G, HUNZIKER P et al.: Evidence for endothelin-1-mediated vasoconstriction in severe chronic heart failure. Lancet (1995) 346:732–736.
  • SOTSCH G, KIOWSKI W, YAN X-W et al.: Short-term oral endothelin-receptor antagonist therapy in conventionally treated patients with symptomatic severe chronic heart failure. Circulation (1998) 98:2262–2268.
  • WEBER C, GASSER R, HOPFGARTNER G: Absorption, excretion, and metabolism of the endothelin receptor antagonist bosentan in healthy male subjects. Drug Metabol Dispos. (1999) 27:810–815.
  • WEBER C, SCHMITT R, BIRNBOECK H et al.: Multiple-dose pharmacokinetics, safety, and tolerability of bosentan, an endothelin receptor antagonist, in healthy male volunteers. Clin. Pharmacol (1999) 39:703–714.
  • WEBER C, SCHMITT R, BIRNBOECK H et al.: Pharmacokinetics and pharmacodynamics of the endothelin-receptor antagonist bosentan in healthy human subjects. Clin. Pharmacol Thec (1996) 60:124–137.
  • WEBER C, BANKEN L, BIRNBOECK H, SCHULZ R: Effect of the endothelin-receptor antagonist bosentan on the pharmacokinetics and pharmacodynamics of warfarin. Clin. Pharmacol (1999) 39:847–854.
  • WEBER C, BANKEN L, BIRNBOECK H, NAVE S, SCHULZ R: The effect of bosentan on the pharmacokinetics of digoxin in healthy male subjects. Br. Clin. Pharmacol (1999) 47:701–706.
  • VAN GIERSBERGEN PLM, CLOZEL M, BODIN F: A drug interaction study between bosentan and ketoconazole and losartan. [Abstract] Clin. Pharmacol Ther. (2001) 69:P67.
  • DINGEMANSE J, BODIN F, WEIDEKAMM E, KUTZ K, VAN GIERSBERGEN P: Influence of food intake and formulation on the pharmacokinetics and metabolism of bosentan, a dual endothelin receptor antagonist. Clin. Pharmacol (2002) 42:283–289.
  • CHANNICK RN, SIMONNEAU G, SITBON 0 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.
  • ••Report of the first study of an ERA in patients with pulmonary hypertension.
  • RUBIN LJ, BADESCH DB, BARST RJ et al.: Bosentan therapy for pulmonary arterial hypertension. N Engl. I Med. (2002) 346:896–903.
  • ••Report of the pivotal double-blind, placebo-controlled trial of bosentan in patients with pulmonary hypertension.
  • PACKER M, CASPI A, CHARLON V et al: Multicenter, double-blind, placebo-controlled study of long-term endothelin blockade with bosentan in chronic heart failure — results of the REACH-1 trial. Circulation (1998) 98(Suppl.):I–3.
  • PACKER M. Effects of the endothelin receptor antagonist bosentan on the morbidity and mortality in patients with chronic heart failure: results of the ENABLE 1 and 2 trial program. American College of Cardiology 51st Annual Scientific Session, Atlanta, GA. March 19, 2002.
  • KRUM H, CHARLON V, WIDMANN T, PACKER M: Long-term, open-label experience with an endothelin receptor antagonist, bosentan, in patients with severe chronic heart failure. [Abstract] Circulation (1999) 100\(Suppl. 41646.
  • MYLONA P, CLELAND JGF, on behalf of the CARDIO.NET EDITORIAL TEAM: Update of REACH-1 and MERIT-HF clinical trials in heart failure. Ear: I Heart Failure (1999) 1:197–200.
  • BELCH JJF: Raynaud's phenomenon. CurcOpin. Rheumatol (1989) 1:490–498.
  • TAMAKI T, MORI S, TAKEHARA K. Epidemiological study of patients with systemic sclerosis in Tokyo. Arch. Dermatol Res. (1991) 283:366–371.

Websites

  • http://www.who.int/ncd/cvd/pph.html Executive summary from the World Symposium on Primary Pulmonary Hypertension (1998).
  • •Overview of the current understanding of primary pulmonary hypertension.
  • http://www.pha-uk.com/info-whatisit.htm Pulmonary Hypertension Association (UK) website, What Is It? (2001).

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.