Safety and tolerability of bosentan in the management of pulmonary arterial hypertension

Drug Design, Development and Therapy

Volumn , Issue 3, 2009, Pages 111-118

  Roberts, Kari E ^a   Preston, Ioana R ^a  

^a TUFTS MEDICAL CENTER   (United States)

Author keywords

Bosentan; Endothelin receptor antagonists; Pulmonary arterial hypertension

Indexed keywords

BOSENTAN; CYCLOSPORIN A; ENDOTHELIN 1; ENDOTHELIN A RECEPTOR; GLIBENCLAMIDE; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; ORAL CONTRACEPTIVE AGENT; PHOSPHODIESTERASE V INHIBITOR; PROSTACYCLIN DERIVATIVE; PYRROLE DERIVATIVE; SILDENAFIL; WARFARIN;

BLOOD VESSEL TONE; CLINICAL TRIAL; DISEASE CLASSIFICATION; DRUG ANTAGONISM; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DOSE INCREASE; DRUG DOSE REDUCTION; DRUG EFFICACY; DRUG SAFETY; DRUG TOLERABILITY; DRUG WITHDRAWAL; HUMAN; LEG EDEMA; LIVER TOXICITY; MONOTHERAPY; NOSE CONGESTION; PULMONARY HYPERTENSION; REVIEW; SIDE EFFECT; TREATMENT DURATION; WEIGHT GAIN;

EID: 77953668705     PISSN: None     EISSN: 11778881     Source Type: Journal    
DOI: None     Document Type: Review

References (58)

1. Rubin LJ. Primary pulmonary hypertension. N Engl J Med. 1997;336(2):111-117.
2. Yanagisawa M, Inoue A, Ishikawa T, et al. Primary structure, synthesis, and biological activity of rat endothelin, an endothelium-derived vasoconstrictor peptide. Proc Natl Acad Sci U S A. 1988;85(18): 6964-6967. (Pubitemid 18223558)
3. Clozel M, Breu V, Gray GA, et al. Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. J Pharmacol Exp Ther. 1994;270(1):228-235. (Pubitemid 24229632)
4. Giaid A, Yanagisawa M, Langleben D, et al. Expression of endothelin-1 in the lungs of patients with pulmonary hypertension. N Engl J Med. 1993;328(24):1732-1739. (Pubitemid 23170122)
5. Jankov RP, Kantores C, Belcastro R, Yi M, Tanswell AK. Endothelin-1 inhibits apoptosis of pulmonary arterial smooth muscle in the neonatal rat. Pediatr Res. 2006;60(3):245-251. (Pubitemid 44267733)
6. Shichiri M, Kato H, Marumo F, Hirata Y. Endothelin-1 as an autocrine/ paracrine apoptosis survival factor for endothelial cells. Hypertension. 1997;30(5):1198-1203. (Pubitemid 27476179)
7. Humbert M, Morrell NW, Archer SL, et al. Cellular and molecular pathobiology of pulmonary arterial hypertension. J Am Coll Cardiol. 2004;43(12 Suppl S):13S-24S. (Pubitemid 38759713)
8. Michelakis ED. Spatio-temporal diversity of apoptosis within the vascular wall in pulmonary arterial hypertension: heterogeneous BMP signaling may have therapeutic implications. Circ Res. 2006;98(2):172-175.
9. Voelkel NF, Cool C, Lee SD, Wright L, Geraci MW, Tuder RM. Primary pulmonary hypertension between inflammation and cancer. Chest. 1998;114(3 Suppl):225S-230S. (Pubitemid 28435972)
10. Arai H, Hori S, Aramori I, Ohkubo H, Nakanishi S. Cloning and expression of a cDNA encoding an endothelin receptor. Nature. 1990;348(6303):730-732. (Pubitemid 120015147)
11. Sakurai T, Yanagisawa M, Takuwa Y, et al. Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor. Nature. 1990;348(6303):732-735. (Pubitemid 120015148)
12. Evans AM, Cobban HJ, Nixon GF. ET(A) receptors are the primary mediators of myofilament calcium sensitization induced by ET-1 in rat pulmonary artery smooth muscle: a tyrosine kinase independent pathway. Br J Pharmacol. 1999;127(1):153-160.
13. Davie N, Haleen SJ, Upton PD, et al. ET(A) and ET(B) receptors modulate the proliferation of human pulmonary artery smooth muscle cells. Am J Respir Crit Care Med. 2002;165(3):398-405. (Pubitemid 34118516)
14. de Nucci G, Thomas R, D'Orleans-Juste P, et al. 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 U S A. 1988;85(24):9797-9800. (Pubitemid 19027212)
15. Dupuis J, Goresky CA, Fournier A. Pulmonary clearance of circulating endothelin-1 in dogs in vivo: exclusive role of ETB receptors. J Appl Physiol. 1996;81(4):1510-1515. (Pubitemid 26349600)
16. Dupuis J, Stewart DJ, Cernacek P, Gosselin G. Human pulmonary circulation is an important site for both clearance and production of endothelin-1. Circulation. 1996;94(7):1578-1584. (Pubitemid 26320261)
17. van Giersbergen PL, Popescu G, Bodin F, Dingemanse J. Influence of mild liver impairment on the pharmacokinetics and metabolism of bosentan, a dual endothelin receptor antagonist. J Clin Pharmacol. 2003;43(1):15-22. (Pubitemid 36015438)
18. Weber C, Schmitt R, Birnboeck H, et al. Pharmacokinetics and pharmacodynamics of the endothelin-receptor antagonist bosentan in healthy human subjects. Clin Pharmacol Ther. 1996;60(2):124-137. (Pubitemid 26348226)
19. 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(3):283-289. (Pubitemid 34163474)
20. Dingemanse J, van Giersbergen PL. Clinical pharmacology of bosentan, a dual endothelin receptor antagonist. Clin Pharmacokinet. 2004;43(15):1089-1115. (Pubitemid 40013178)
21. 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(8):847-854. (Pubitemid 30629445)
22. Treiber A, Schneiter R, Hausler 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(8):1400-1407. (Pubitemid 47121782)
23. Burgess G, Hoogkamer H, Collings L, Dingemanse J. Mutual pharmacokinetic interactions between steady-state bosentan and sildenafil. Eur J Clin Pharmacol. 2008;64(1):43-50.
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(1):107-112. (Pubitemid 40942789)
25. Wrishko RE, Dingemanse J, Yu A, Darstein C, Phillips DL, Mitchell MI. Pharmacokinetic interaction between tadalafil and bosentan in healthy male subjects. J Clin Pharmacol. 2008;48(5):610-618.
26. 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(3):113-118. (Pubitemid 43338011)
27. 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(4): 223-231. (Pubitemid 32382504)
28. Mano Y, Usui T, Kamimura H. Effects of bosentan, an endothelin receptor antagonist, on bile salt export pump and multidrug resistance-associated protein 2. Biopharm Drug Dispos. 2007;28(1):13-18. (Pubitemid 46165160)
29. Rubin LJ, Badesch DB, Barst RJ, et al. Bosentan therapy for pulmonary arterial hypertension. N Engl J Med. 2002;346(12):896-903. (Pubitemid 34984638)
30. 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(2):338-344. (Pubitemid 47194187)
31. Hoeper MM, Halank M, Marx C, et al. Bosentan therapy for portopulmonary hypertension. Eur Respir J. 2005;25(3):502-508.
32. Williamson DJ, Wallman LL, Jones R, et al. Hemodynamic effects of Bosentan, an endothelin receptor antagonist, in patients with pulmonary hypertension. Circulation. 2000;102(4):411-418. (Pubitemid 30490679)
33. Channick RN, 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):1119-1123. (Pubitemid 32971843)
34. Galie N, Hinderliter AL, Torbicki A, et al. Effects of the oral endothelin-receptor antagonist bosentan on echocardiographic and doppler measures in patients with pulmonary arterial hypertension. J Am Coll Cardiol. 2003;41(8):1380-1386. (Pubitemid 36439000)
35. Sitbon O, Badesch DB, Channick RN, et al. Effects of the dual endothelin receptor antagonist bosentan in patients with pulmonary arterial hypertension: a 1-year follow-up study. Chest. 2003;124(1): 247-254. (Pubitemid 36851359)
36. McLaughlin VV, Sitbon O, Badesch DB, et al. Survival with first-line bosentan in patients with primary pulmonary hypertension. Eur Respir J. 2005;25(2):244-249. (Pubitemid 40246523)
37. Sitbon O, McLaughlin VV, Badesch DB, et al. Survival in patients with class III idiopathic pulmonary arterial hypertension treated with first-line oral bosentan compared with an historical cohort of patients started on i.v. epoprostenol. Thorax. 2005. (Pubitemid 41705471)
38. Galie 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(9630):2093-2100. (Pubitemid 351902178)
39. Barst RJ, Ivy D, Dingemanse J, et al. Pharmacokinetics, safety, and efficacy of bosentan in pediatric patients with pulmonary arterial hypertension. Clin Pharmacol Ther. 2003;73(4):372-382. (Pubitemid 36403597)
40. Sitbon O, Gressin V, Speich R, et al. Bosentan for the treatment of human immunodeficiency virus-associated pulmonary arterial hypertension. Am J Respir Crit Care Med. 2004;170(11): 1212-1217. (Pubitemid 39577380)
41. Degano B, Yaici A, Le Pavec J, et al. Long-term effects of bosentan in patients with HIV-associated pulmonary arterial hypertension. Eur Respir J. 2009;33(1):92-98.
42. Galie N, Beghetti M, Gatzoulis MA, et al. Bosentan therapy in patients with Eisenmenger syndrome: a multicenter, double-blind, randomized, placebo-controlled study. Circulation. 2006;114(1):48-54. (Pubitemid 44305274)
43. Ulrich S, Speich R, Domenighetti G, et al. Bosentan therapy for chronic thromboembolic pulmonary hypertension. A national open label study assessing the effect of Bosentan on haemodynamics, exercise capacity, quality of life, safety and tolerability in patients with chronic thromboembolic pulmonary hypertension (BOCTEPH-Study). Swiss Med Wkly. 2007;137(41-42):573-580.
44. Bonderman D, Nowotny R, Skoro-Sajer N, et al. Bosentan therapy for inoperable chronic thromboembolic pulmonary hypertension. Chest. 2005;128(4):2599-2603. (Pubitemid 41507615)
45. Hoeper MM, Kramm T, Wilkens H, et al. Bosentan therapy for inoperable chronic thromboembolic pulmonary hypertension. Chest. 2005;128(4):2363-2367. (Pubitemid 41507580)
46. Kaluski E, Cotter G, Leitman M, et al. Clinical and hemodynamic effects of bosentan dose optimization in symptomatic heart failure patients with severe systolic dysfunction, associated with secondary pulmonary hypertension - a multi-center randomized study. Cardiology. 2008;109(4):273-280. (Pubitemid 351328923)
47. Stolz D, Rasch H, Linka A, et al. A randomised, controlled trial of bosentan in severe COPD. Eur Respir J. 2008;32(3):619-628.
48. Hoeper MM, Taha N, Bekjarova A, Gatzke R, Spiekerkoetter E. Bosentan treatment in patients with primary pulmonary hypertension receiving nonparenteral prostanoids. Eur Respir J. 2003;22(2):330-334. (Pubitemid 36987006)
49. Humbert M, Barst RJ, Robbins IM, et al. Combination of bosentan with epoprostenol in pulmonary arterial hypertension: BREATHE-2. Eur Respir J. 2004;24(3):353-359. (Pubitemid 39232254)
50. McLaughlin VV, Oudiz RJ, Frost A, et al. Randomized study of adding inhaled iloprost to existing bosentan in pulmonary arterial hypertension. Am J Respir Crit Care Med. 2006;174(11):1257-1263. (Pubitemid 44924827)
51. Hoeper MM, Leuchte H, Halank M, et al. Combining inhaled iloprost with bosentan in patients with idiopathic pulmonary arterial hypertension. Eur Respir J. 2006;28(4):691-694. (Pubitemid 46331988)
52. Kim NH, Channick RN, Rubin LJ. Successful withdrawal of long-term epoprostenol therapy for pulmonary arterial hypertension. Chest. 2003;124(4):1612-1615. (Pubitemid 37290078)
53. Ivy DD, Doran A, Claussen L, Bingaman D, Yetman A. Weaning and discontinuation of epoprostenol in children with idiopathic pulmonary arterial hypertension receiving concomitant bosentan. Am J Cardiol. 2004;93(7):943-946. (Pubitemid 38429615)
54. Steiner MK, Preston IR, Klinger JR, et al. Conversion to bosentan from prostacyclin infusion therapy in pulmonary arterial hypertension: a pilot study. Chest. 2006;130(5):1471-1480. (Pubitemid 44786742)
55. Suleman N, Frost AE. Transition from epoprostenol and treprostinil to the oral endothelin receptor antagonist bosentan in patients with pulmonary hypertension. Chest. 2004;126(3):808-815. (Pubitemid 39258035)
56. McGoon MD, Barst RJ, Doyle RL, Liou TG, Miller D, Feldkircher K. Reveal Registry: treatment history and treatment at baseline. Chest Meeting Abstracts. Chest. 2007;132:631. Available online at http:// meeting.chestjournal.org/cgi/ search?fulltext=mcgoon&sendit=Enter &volume=132&issue= 4&journalcode=chestmtg.
57. Badesch DB, Abman SH, Simonneau G, Rubin LJ, McLaughlin VV. Medical therapy for pulmonary arterial hypertension: updated ACCP evidence-based clinical practice guidelines. Chest. 2007;131(6):1917-1928. (Pubitemid 46981654)
58. Simonneau G, Galie N, Rubin LJ, et al. Clinical classification of pulmonary hypertension. J Am Coll Cardiol. 2004;43(12 Suppl S):5S-12S.