479
Views
19
CrossRef citations to date
0
Altmetric
Drug Safety Evaluations

Safety and efficacy evaluation of ambrisentan in pulmonary hypertension

, MD, , MD, , MD &
Pages 1003-1011 | Published online: 04 Aug 2012

Bibliography

  • Simonneau G, Robbins I, Beghetti M, Updated clinical classification of pulmonary hypertension. J Am Coll Cardiol 2009;54:S43-54
  • Rich S. Pulmonary hypertension. In: Braunwald E, Zipes DP, Libby P, editors. Heart disease: a textbook of cardiovascular medicine. WB Saunders; Philadelphia, PA: 2001. p. 1912-29
  • D’Alonzo GE, Barst RJ, Ayres SM, Survival in patients with primary pulmonary hypertension. Results from a national prospective registry. Ann Intern Med 1991;115:343-9
  • Humbert M, Morrell NW, Archer SL, Cellular and molecular pathobiology of pulmonary arterial hypertension. J Am Coll Cardiol 2004;43:S13-24
  • Rubens C, Ewert R, Halank M, Big endothelin-1 and endothelin-1 plasma levels are correlated with the severity of primary pulmonary hypertension. Chest 2001;120:1562-9
  • Giaid A, Yanagisawa M, Langleben D, Expression of endothelin-1 in the lungs of patients with pulmonary hypertension. N Engl J Med 1993;328:1732-9
  • Sakurai T, Cloning of a cDNA encoding a non-isopeptide selective subtype of the endothelin receptor. Nature 1990;348:732-5
  • Hirata Y, Emori T, Eguchi S. Endothelin receptor subtype B mediates synthesis of nitric oxide by cultured bovine endothelial cells. J Clin Invest 1993;91:1367-73
  • deNucci G, Thomas R, D Orleans-Juste P, 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 1988;85:9797-800
  • Filep J, Herman F, Battstini B, Antiaggregatory and hypotensive effects of endothelin-1 in beagle dogs: role for prostacyclin. J Cardiovasc Pharmacol 1991;17:S216-18
  • Masaki T. Possible role of endothelin in endothelial regulation of vascular tone. Ann Rev Pharmacol Toxicol 1995;35:235-55
  • Rubin LJ, Badesch DB, Barst RJ, Bosentan therapy for pulmonary arterial hypertension. N Engl J Med 2002;346:896-0
  • Barst RJ, Langleben D, Frost A, Sitaxsentan therapy for pulmonary arterial hypertension. Am J Respir Crit Care Med 2004;169:441-7
  • Galiè N, Olschewski H, Oudiz RJ, 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;117:3010-19
  • European Medicines Agency. Thelin (sitaxentan) to be withdrawn due to cases of unpredictable serious liver injury [press release]. December 20, 2010
  • Riechers H, Albrecht HP, Amberg W, Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists. J Med Chem 1996;39:2123-8
  • Casserly B, Klinger JR. Ambrisentan for treatment of pulmonary arterial hypertension. Drug Des, Dev Ther 2008;2:265-80
  • Dupuis J, Hoeper MM. Endothelin receptor antagonists in pulmonary arterial hypertension. Eur Respir J 2008;31:407-15
  • Galiè N, Badesch D, Oudiz R, Ambrisentan therapy for pulmonary arterial hypertension. J Am Coll Cardiol 2005;46:529-35
  • Barst RJ. A review of pulmonary arterial hypertension: role of ambrisentan. Vasc Health Risk Manag 2007;3:11-22
  • Hartman JC, Brouwer K, Mandagere A, Evaluation of the endothelin receptor antagonists ambrisentan, darusentan, bosentan, and sitaxsentan as substrates and inhibitors of hepatobiliary transporters in sandwich-cultured human hepatocytes. Can J Physiol Pharmacol 2010;88:682-91
  • Galiè N, Keogh AM, Frost A, Ambrisentan long-term safety and efficacy in pulmonary arterial hypertension-one year follow up. Proc Am Thorac Soc 2005;2:A299
  • Badesch DB, Feldman J Keogh A, ARIES-3: ambrisentan therapy in a diverse population of patients with pulmonary hypertension. Cardiovasc Ther 2011;00:1-7
  • Oudiz RJ, Galiè N, Olschewski H, Long-term ambrisentan therapy for the treatment of pulmonary arterial hypertension. J Am Coll Cardiol 2009;21:1971-81
  • Klinger JR, Oudiz RJ, Spence R, Long-term pulmonary hemodynamic effects of ambrisentan in pulmonary arterial hypertension. Am J Cardiol 2011;108:302-7
  • McGoon MD, Frost AE, Oudiz RJ, Ambrisentan therapy in patients with pulmonary arterial hypertension who discontinued bosentan or sitaxsentan due to liver function test abnormalities. Chest 2009;135:122-9
  • Kenyon KW, Nappi JM. Bosentan for the treatment of pulmonary arterial hypertension. Ann Pharmacother 2003;37:1055-62
  • Paul GA, Gibbs JS, Boobis AR, Bosentan decreases the plasma concentration of sildenafil when coprescribed in pulmonary hypertension. Br J Clin Pharmacol 2005;60:107-12
  • Treiber A, Schneiter R, Häusler S, Stieger B. 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 2007;35:1400-7
  • Binet I, Wallnöfer A, Weber C, Renal hemodynamics and pharmacokinetics of bosentan with and without cyclosporine A. Kidney Int 2000;57:224-31
  • van Giersbergen PL, Treiber A, Clozel M, In vivo and in vitro studies exploring the pharmacokinetic interaction between bosentan, a dual endothelin receptor antagonist, and glyburide. Clin Pharmacol Ther 2002;71:253-62
  • van Giersbergen PL, Halabi A, Dingemanse J. Pharmacokinetic interaction between bosentan and the oral contraceptives norethisterone and ethinyl estradiol. Int J Clin Pharmacol Ther 2006;44:113-18
  • Dingemanse J, Schaarschmidt D, van Giersbergen PL. Investigation of the mutual pharmacokinetic interactions between bosentan, a dual endothelin receptor antagonist, and simvastatin. Clin Pharmacokinet 2003;42:293-301
  • Dingemanse J, van Giersbergen PL, Patat A, Nilsson PN. Mutual pharmacokinetic interactions between bosentan and lopinavir/ritonavir in healthy participants. Antivir Ther 2010;15:157-63
  • van Giersbergen PL, Treiber A, Schneiter R, Inhibitory and inductive effects of rifampin on the pharmacokinetics of bosentan in healthy subjects. Clin Pharmacol Ther 2007;81:414-19; Erratum in: Clin Pharmacol Ther 2007; 81:460
  • Dingemanse J, van Giersbergen PL. Clinical pharmacology of bosentan, a dual endothelin receptor antagonist. Clin Pharmacokinet 2004;43:1089-115
  • Dufton C, Gerber M, Yin O, No clinically relevant pharmacokinetic interaction between ambrisentan and sildenafil. Chest 2006;130:254S
  • Gerber MJ, Dufton C, Pentikis H, Ambrisentan has no clinically relevant effect on the pharmacokinetics or pharmacodynamics of warfarin. Chest 2006;130:256S
  • Spence R, Mandagere A, Harrison B, No clinically relevant pharmacokinetic and safety interactions of ambrisentan in combination with tadalafil in healthy volunteers. J Pharm Sci 2009;98:4962-74
  • Richards DB, Walker GA, Mandagere A, Effect of ketoconazole on the pharmacokinetic profile of ambrisentan. J Clin Pharmacol 2009;49:719-24
  • Richards DB, Spence R, Mandagere A, Effects of multiple doses of ambrisentan on the pharmacokinetics of a single dose of digoxin in healthy volunteers. J Clin Pharmacol 2011;51:102-6
  • Spence R, Mandagere A, Walker G, Effect of steady-state ambrisentan on the pharmacokinetics of a single dose of the oral contraceptive norethindrone (norethisterone) 1 mg/ethinylestradiol 35 microg in healthy subjects: an open-label, single-sequence, single-centre study. Clin Drug Investig 2010;30:313-24
  • Harrison B, Magee MH, Mandagere A, Effects of rifampicin (rifampin) on the pharmacokinetics and safety of ambrisentan in healthy subjects: a single-sequence, open-label study. Clin Drug Investig 2010;30:875-85
  • Spence R, Mandagere A, Richards DB, Potential for pharmacokinetic interactions between ambrisentan and cyclosporine. Clin Pharmacol Ther 2010;88:513-20
  • Ben-Yehuda O, Pizzuti D, Brown A, Long-term hepatic safety of ambrisentan in patients with pulmonary arterial hypertension. J Am Coll Cardiol 2012; published online May 9 2012; doi:10.1016/j.jacc.2012.03.025
  • Channick RN, Simonneau G, Sitbon O, Effect of the dual endothelin-receptor antagonist bosentan in patients with pulmonary hypertension: a randomised placebo-controlled study. Lancet 2001;358:1119-23
  • Barst RJ, Langleben D, Badesch D, Treatment of pulmonary arterial hypertension with the selective endothelin-A receptor antagonist sitaxsentan. J Am Coll Cardiol 2006;47:2049-56
  • Sitbon O, Gressin V, Speich R, Bosentan for the treatment of human immunodeficiency virus–associated pulmonary arterial hypertension. Am J Respir Crit Care Med 2004;170:1212-17
  • Califf RM, Adams KF, McKenna WJ, A randomized controlled trial of epoprostenol therapy for severe congestive heart failure: the Flolan International Randomized Survival Trial (FIRST). Am Heart J 1997;134:44-54
  • Packer M, McMurray J, Massie BM, Clinical effects of endothelin receptor antagonism with bosentan in patients with severe chronic heart failure: results of a pilot study. J Card Fail 2005;11:12-20
  • Lewis GD, Shah R, Shahzad K, Sildenafil improves exercise capacity and quality of life in patients with systolic heart failure and secondary pulmonary hypertension. Circulation 2007;116:1555-62
  • Galiè N, Beghetti M, Gatzoulis MA, Bosentan therapy in patients with Eisenmenger syndrome: a multicenter, double-blind, randomized, placebo-controlled study. Circulation 2006;114:48-54
  • Jaïs X, D'Armini AM, Jansa P, Bosentan for treatment of inoperable chronic thromboembolic pulmonary hypertension: BENEFiT (Bosentan Effects in iNopErable Forms of chronIc Thromboembolic pulmonary hypertension), a randomized, placebo-controlled trial. J Am Coll Cardiol 2008;52:2127-34
  • Iglarz M, Binkert B, Morrison K, Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. J Pharmacol Exp Ther 2008;327:736-45

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.