Bosentan for the treatment of pulmonary arterial hypertension

Annals of Pharmacotherapy

Volumn 37, Issue 7-8, 2003, Pages 1055-1062

  Kenyon, Kenneth W ^a   Nappi, Jean M ^a  

^a MEDICAL UNIVERSITY OF SOUTH CAROLINA   (United States)

Author keywords

Bosentan; Pulmonary hypertension; Ro 47 0203

Indexed keywords

BOSENTAN; CONTRACEPTIVE AGENT; CYCLOSPORIN; CYTOCHROME P450; ENDOTHELIN RECEPTOR ANTAGONIST; GLIBENCLAMIDE; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; KETOCONAZOLE; PLACEBO; PROSTACYCLIN; SIMVASTATIN; UNIPROST; WARFARIN;

BIRTH DEFECT; CARDIOPULMONARY HEMODYNAMICS; CLINICAL TRIAL; DRUG CLEARANCE; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG LABELING; DRUG MECHANISM; DRUG METABOLISM; DRUG SAFETY; EXERCISE TOLERANCE; FLUSHING; FOOD AND DRUG ADMINISTRATION; HEADACHE; HUMAN; HYPOTENSION; JAW DISEASE; LEG EDEMA; LIVER INJURY; MEDLINE; MULTICENTER STUDY; MYALGIA; OUTCOMES RESEARCH; PAIN; PATIENT COUNSELING; PRACTICE GUIDELINE; PRIORITY JOURNAL; PULMONARY HYPERTENSION; QUALITY OF LIFE; REVIEW; RHINOPHARYNGITIS; WORLD HEALTH ORGANIZATION;

EID: 0038441800     PISSN: 10600280     EISSN: None     Source Type: Journal    
DOI: 10.1345/aph.1C256     Document Type: Review

References (54)

1. Mealy NE, Bayes M, del Fresno M. Bosentan. Drugs Fut 2001;26:1149-54.
2. Klings ES, Farber HW. Current management of primary pulmonary hypertension. Drugs 2001;61:1945-56.
3. Rubin LJ. Primary pulmonary hypertension. N Engl J Med 1997;336:111-7.
4. Rubin LJ, Badesch DB, Barst RJ, Galie N, Black CM, Keogh A, et al. Bosentan therapy for pulmonary arterial hypertension. N Engl J Med 2002;346:896-903.
5. Ungerer RG, Tashkin DP, Furst D, Clements PJ, Gong H Jr, Bein M. et al. Prevalence and clinical correlates of pulmonary arterial hypertension in progressive systemic sclerosis. Am J Med 1983;75:65-74.
6. Rich S. A new classification of pulmonary hypertension. Advances in Pulmonary Hypertension [serial online]. www.phassociation.org/Medical/spring_2002/PH_Classification.asp (accessed 2002 Sept 22).
7. Ergul A. Endothelin-1 and endothelin receptor antagonist as potential cardiovascular therapeutic agents. Pharmacotherapy 2002;22:55-65.
8. Borg GA. Psychophysical bases of perceived exertion. Med Sci Sports Exerc 1982;14:377-81.
9. Gibbons RJ, Balady GJ, Beasley JW, Bricker JT, Duvernoy WFC, Froelicher VF, et al. ACC/AHA guidelines for exercise testing: a report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on Exercise Testing). J Am Coll Cardiol 1997;30:260-315.
10. Rich S, ed. Primary pulmonary hypertension: executive summary from the world symposium. Geneva: World Health Organization, 1998. www.who. int/ncd/cvd/pph.html (accessed 2002 Apr 27).
11. Herner SJ, Mauro LS. Epoprostenol in primary pulmonary hypertension. Ann Pharmacother 1999;33:340-7.
12. Barst RJ, Rubin LJ, Long WA, McGoon MD, Rich S, Badesch DB, et al. A comparison of continuous intravenous epoprostenol (prostacyclin) with conventional therapy for primary pulmonary hypertension. N Engl J Med 1996;334:296-301.
13. Badesch DB, Tapson VF, McGoon MD, Brundage BH, Rubin LJ, Wigley FM, et al. Continuous intravenous epoprostenol for pulmonary hypertension due to the scleroderma spectrum of disease. Ann Intern Med 2000;132:425-34.
14. Weber C, Schmitt R, Birnboeck H, Hopfgartner G, van Marle SP, Peeters PAM, et al. Pharmacokinetics and pharmacodynamics of the endothelin-receptor antagonist bosentan in healthy human subjects. Clin Pharmacol Ther 1996;60:124-37.
15. Package insert. Tracleer (bosentan). South San Francisco: Actelion Pharmaceuticals, May 2002.
16. Weber C, Gasser R, Hopfgartner G. Absorption, excretion, and metabolism of the endothelin receptor antagonist bosentan in healthy male subjects. Drug Metab Dispos 1999;27:810-5.
17. Weber C, Schmitt R, Birnboeck H, Hopfgartner G, Eggers H, Meyer J, et al. Multiple-dose pharmacokinetics, safety, and tolerability of bosentan, an endothelin receptor antagonist, in healthy male volunteers. J Clin Pharmacol 1999;39:703-14.
18. Roux S, Breu V, Ertel S, Clozel M. Endothelin antagonism with bosentan: a review of potential applications. J Mol Med 1999;77:364-76.
19. Clozel M, Breu V, Gray GA, Kalina B, Loffler BM, Burri K. Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. J Pharmacol Exp Ther 1994;270:228-35.
20. Williamson JD, Wallman LL, Jones R, Keogh A, Scroope F, Penny R, et al. Hemodynamic effects of bosentan, an endothelin receptor antagonist, in patients with pulmonary hypertension. Circulation 2000;102:411-8.
21. Maguire JJ, Davenport AP. ETA receptor-mediated constrictor responses to endothelin peptides in human blood vessels in vitro. Br J Pharmacol 1995;115:191-7.
22. Krum H, Viskoper RJ, 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;338:784-90.
23. Giaid A, Yanagisawa M, Langleben D, Michel RP, Levy R, Shennib H, et al. Expression of endothelin-1 in the lungs of patients with primary pulmonary hypertension. N Engl J Med 1993;328:1732-9.
24. Wei CM, Lerman A, Rodeheffer RJ, McGregor CGA, Brandt RR, Wright S, et al. Endothelin in human congestive heart failure. Circulation 1994;89:1580-6.
25. Chen SJ, Chen YF, Meng QC, Durand J, Dicarlo VS, Oparil S. Endothelin-receptor antagonist bosentan prevents and reverses hypoxic pulmonary hypertension in rats. J Appl Physiol 1995;79:2122-31.
26. Park SH, Saleh D, Giaid A, Michel RP. Increased endothelin-1 in bleo mycin-induced pulmonary fibrosis and the effect of an endothelin receptor antagonist. Am J Respir Crit Care Med 1997;156:600-8.
27. B receptors. Br J Pharmacol 1995;115:227-36.
28. 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. J Clin Pharmacol 2002;42:283-9.
29. Channick RN, Simonneau G, Sitbon O, Robbins IM, Frost A, Tapson VF, et al. Effects of the dual endothelin-receptor antagonist bosentan in patients with pulmonary hypertension: a randomized placebo-controlled study. Lancet 2001;358:1119-23.
30. Actelion Ltd. media release. Actelion announces U.S. commercial availability of Tracleer (bosentan) tablets - first oral treatment for pulmonary arterial hypertension ready to ship to patients. December 5, 2001. www. tracleer.com/tracleer_website/hcp/US_Commercial_Release_Final_5_Dec_ 2001.pdf (accessed 2002 May 15).
31. FDA/Center for Drug Evaluation and Research. New and generic drug approvals: Tracleer. www.fda.gov/cder/approval/index.htm (accessed 2002 May 15).
32. van Giersbergen PLM, Treiber A, Clozel M, Bodin F, Dingemanse J. 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.
33. Packer M. Multicentre, double-blind, placebo-controlled study of long-term endothelin blockade with bosentan in chronic heart failure - results of the REACH-1 trial (abstract). Circulation 1998;98(suppl):1-3.
34. Fattinger K, Funk C, Pantze M, Weber C, Reichen J, Stieger B, et al. The endothelin antagonist bosentan inhibits the canalicular bile salt export pump: a potential mechanism for hepatic adverse reactions. Clin Pharmacol Ther 2001;69:223-31.
35. Weber C, Banken L, Birnboeck H, Schulz R. Effect of the endothelin-receptor antagonist bosentan on the pharmacokinetics and pharmacodynamics of warfarin. J Clin Pharmacol 1999;39:847-54.
36. Olschewski H, Simonneau G, Galie N, Higenbottam T, Naeije R, Rubin LJ, et al. Inhaled iloprost for severe pulmonary hypertension. N Engl J Med 2002;347:322-9.
37. Galie N, Humbert M, Vachiery JL, Vizza CD, Kneussl M, Manes A, et al. Effects of beraprost sodium, an oral prostacyclin analogue, in patients with pulmonary arterial hypertension: a randomized, double-blind, placebo-controlled trial. J Am Coll Cardiol 2002;39:1496-502.
38. Givertz MM, Colucci WS, LeJemtel TH, Gottlieb SS, Hare JM, Slawsky MT, et al. Acute endothelin A receptor blockade causes selective pulmonary vasodilation in patients with chronic heart failure. Circulation 2000;101:2922-7.
39. Barst RJ, Rich S, Widlitz A, Horn EM, McLaughlin V, McFarlin J. Clinical efficacy of sitaxsentan, an endothelin-A receptor antagonist, in patients with pulmonary arterial hypertension. Chest 2002;121:1860-8.
40. Package insert. Flolan (epoprostenol). Research Triangle Park, NC: GlaxoWellcome, August 1999.
41. Pass SE, Dusing ML. Current and emerging therapy for primary pulmonary hypertension. Ann Pharmacother 2002;36:1414-23. DOI 10.1345/aph.1C015
42. Simonneau G, Barst RJ, Galie N, Naeije R, Rich S, Bourge RC, et al. Continuous subcutaneous infusion of treprostinil, a prostacyclin analogue, in patients with pulmonary arterial hypertension: a double-blind, randomized, placebo-controlled trial. Am J Respir Crit Care Med 2002;165:800-4.
43. Product information: Remodulin (treprostinil). Research Triangle Park, NC: United Therapeutics Corporation, March 2002.
44. Shapiro SM, Oudiz RJ, Cao T, Romano MA, Beckman XJ, Goegiou D, et al. Primary pulmonary hypertension: improved long-term effects and survival with continuous intravenous epoprostenol infusion. J Am Coll Cardiol 1997;30:343-9.
45. Benigni A, Remuzzi G. Endothelin antagonists. Lancet 1999;353:133-8.
46. Sutsch G, Stefan C, Yan XW, Strobel W, Rickenbacher P, Hunziker P, et al. Clinical and hemodynamic effects of an orally active endothelin-1 receptor antagonist in patients with refractory chronic heart failure. Circulation 1997;96(suppl):I93-4.
47. Mylona P, Cleland JGF. Update of REACH-1 and MERIT-HF clinical trials in heart failure. Eur J Heart Fail 1999;1:197-200.
48. Kalra PR, Moon JCC, Coats AJS. Do results of the ENABLE (Endothelin Antagonist Bosentan for Lowering Cardiac Events in Heart Failure) study spell the end for non-selective endothelin antagonism in heart failure? Int J Cardiol 2002;85:195-7.
49. Binet I, Wallnoffer A, Weber C, Jones R, Thiel G. Renal hemodynamics and pharmacokinetics of bosentan with and without cyclosporine A. Kidney Int 2000;57:224-31.
50. Oldroyd SD, Haylor JL, Morcos SK. Bosentan, an orally active endothelin antagonist: effect on the renal response to contrast media. Radiology 1995;196:661-5.
51. Wallnofer A, Grosset D, Ohman J. Effects of the endothelin antagonist bosentan in patients with elevated Doppler velocities after aneurysmal SAH. In: Proceedings of the 6th International Conference on Cerebral Vasospasm, Sydney, Australia, May 11-15, 1997.
52. Wenzel RR, Fleisch M, Shaw S, Noll G, Kaufmann U, Schmitt R, et al. Hemodynamic and coronary effects of the endothelin antagonist bosentan in patients with coronary artery disease. Circulation 1998;98:2235-40.
53. Centros new drug reviews. www.discovercentrus.com/drugreviews/tracleer.html (accessed 2002 Jun 13).
54. Cohen HE, ed. 2002 Drug topics redbook. 106th ed. Montvale, NJ: Thomson Medical Economics, 2002.