Bosentan: A review of its use in the management of digital ulcers associated with systemic sclerosis

Drugs

Volumn 69, Issue 14, 2009, Pages 2005-2024

  Dhillon, Sohita ^a  

^a Wolters Kluwer Business ^*  (New Zealand)

Author keywords

[No Author keywords available]

Indexed keywords

ANGIOTENSIN II ANTAGONIST; BOSENTAN; CALCIUM CHANNEL BLOCKING AGENT; CYCLOSPORIN; DIGOXIN; DIPEPTIDYL CARBOXYPEPTIDASE INHIBITOR; ETHINYLESTRADIOL; FLUCONAZOLE; GLIBENCLAMIDE; ITRACONAZOLE; KETOCONAZOLE; LOPINAVIR PLUS RITONAVIR; NEVIRAPINE; NORETHISTERONE ACETATE; PLACEBO; PROSTACYCLIN; RAPAMYCIN; RIFAMPICIN; SILDENAFIL; SIMVASTATIN; TACROLIMUS; WARFARIN;

ABDOMINAL PAIN; ALANINE AMINOTRANSFERASE BLOOD LEVEL; ALTITUDE DISEASE; ANEMIA; ASPARTATE AMINOTRANSFERASE BLOOD LEVEL; BACKACHE; CLINICAL TRIAL; CONSTIPATION; DIARRHEA; DIGITAL ULCER; DIGITAL ULCER DISEASE; DISEASE ASSOCIATION; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG DOSE COMPARISON; DRUG EFFECT; DRUG EFFICACY; DRUG FATALITY; DRUG HALF LIFE; DRUG INDICATION; DRUG MECHANISM; DRUG METABOLISM; DRUG MONITORING; DRUG TOLERABILITY; DRUG WITHDRAWAL; DYSPNEA; EDEMA; ERYTHEMA; ESOPHAGITIS; FEVER; FINGER INJURY; FLUID RETENTION; FLUSHING; GASTROESOPHAGEAL REFLUX; HEART PALPITATION; HEART VENTRICLE TACHYCARDIA; HEMODYNAMIC PARAMETERS; HEMOGLOBIN BLOOD LEVEL; HUMAN; ISCHEMIA; LIVER FUNCTION TEST; LIVER TOXICITY; LUNG EDEMA; MULTIPLE CYCLE TREATMENT; NAUSEA; NONHUMAN; PAIN; POSTMARKETING SURVEILLANCE; QUALITY OF LIFE; REVIEW; RISK FACTOR; SIDE EFFECT; SINGLE DRUG DOSE; SKIN INFECTION; SKIN ULCER; STEADY STATE; SYSTEMIC SCLEROSIS; TERATOGENICITY; TREATMENT CONTRAINDICATION; TREATMENT DURATION; ULCER HEALING; URINARY TRACT INFECTION; VOMITING;

DRUG INTERACTIONS; ENDOTHELIUM, VASCULAR; FINGERS; HUMANS; RECEPTOR, ENDOTHELIN A; SCLERODERMA, SYSTEMIC; SKIN ULCER; SULFONAMIDES; TREATMENT OUTCOME;

EID: 70349162027     PISSN: 00126667     EISSN: 11791950     Source Type: Journal    
DOI: 10.2165/10489160-000000000-00000     Document Type: Review

References (72)

1. Chung L, Fiorentino D. Digital ulcers in patients with systemic sclerosis. Autoimmun Rev 2006; 5 (2): 125-128
2. Charles C, Clements P, Furst DE. Systemic sclerosis: hypothesis-driven treatment strategies. Lancet 2006 May 20; 367 (9523): 1683-1691
3. Chifflot H, Fautrel B, Sordet C, et al. Incidence and prevalence of systemic sclerosis: a systematic literature review. Semin Arthritis Rheum 2008 Feb; 37 (4): 223-235
4. Ramirez A, Varga J. Pulmonary arterial hypertension in systemic sclerosis: clinical manifestations, pathophysiology, evaluation, and management. Treat Respir Med 2004; 3 (6): 339-352
5. Proudman SM, Stevens WM, Sahhar J, et al. Pulmonary arterial hypertension in systemic sclerosis: the need for early detection and treatment. Intern Med J 2007; 37 (7): 485-494
6. Cutolo M, Sulli A, Secchi ME, et al. Nailfold capillaroscopy is useful for the diagnosis and follow-up of autoimmune rheumatic diseases; a future tool for the analysis of microvascular heart involvement? Rheumatology (Oxford) 2006 Oct; 45 Suppl. 4: iv43-iv46
7. Hettema ME, Bootsma H, Kallenberg CGM. Macrovascular disease and atherosclerosis in SSc. Rheumatology (Oxford) 2008 May; 47 (5): 578-583
8. Steen V, Denton CP, Pope JE, et al. Digital ulcers: overt vascular disease in systemic sclerosis. Rheumatology (Oxford) 2009 Jun; 48 Suppl. 3: iii19-24
9. Abraham DJ, Krieg T, Distler J, et al. Overview of pathogenesis of systemic sclerosis. Rheumatology (Oxford) 2009 Jun; 48 Suppl. 3: iii3-7
10. Ferri C, Latorraca A, Catapano G, et al. Increased plasma endothelin-1 immunoreactive levels in vasculitis: a clue to the use of endothelin-1 as a marker of vascular damage? J Hypertens Suppl 1993 Dec; 11 (5): S142-S143
11. European Medicines Agency. Tracleer (bosentan) 62.5mg film-coated tablets: summary of product characteristics [online]. Available from URL: http://www.emea.europa.eu/hum andocs/PDFs/EPAR/tracleer/H-401-PI-en.pdf [Accessed 2009 Aug 6]
12. Actelion Pharmaceuticals US. Inc. Tracleer (bosentan) tablets: US prescribing information [online]. Available from: http://www.accessdata.fda.gov/ drugsatfda-docs/label/2009/ 021290s012lbl.pdf [Accessed 2009 Aug 18]
13. Oldfield V, Lyseng-Williamson KA. Bosentan: a review of its use in pulmonary arterial hypertension and systemic sclerosis. Am J Cardiovasc Drugs 2006; 6 (3): 189-208
14. Prakash A, Perry CM. Bosentan. Am J Cardiovasc Drugs 2002; 2 (5): 335-343
15. Dingemanse J, van Giersbergen PLM. Clinical pharmacology of bosentan, a dual endothelin receptor antagonist. Clin Pharmacokinet 2004; 43 (15): 1089-1115
16. Sfikakis PP, Papamichael C, Stamatelopoulos KS, et al. Improvement of vascular endothelial function using the oral endothelin receptor antagonist bosentan in patients with systemic sclerosis. Arthritis Rheum 2007 Jun; 56 (6): 1985-1993
17. 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 Jul; 270 (1): 228-235
18. Dupuis J, Hoeper MM. Endothelin receptor antagonists in pulmonary arterial hypertension. Eur Respir J 2008 Feb; 31 (2): 407-415
19. Price LC, Howard LS. Endothelin receptor antagonists for pulmonary arterial hypertension: rationale and place in therapy. Am J Cardiovasc Drugs 2008; 8 (3): 171-185
20. Opitz CF, Ewert R,KirchW, et al. Inhibition of endothelin receptors in the treatment of pulmonary arterial hypertension: does selectivity matter? Eur Heart J 2008 Jun 17; 29: 1936-1948
21. Braun-Moscovici Y, Nahir AM, Balbir-Gurman A. Endothelin and pulmonary arterial hypertension. Semin Arthritis Rheum 2004; 34 (1): 442-453
22. Hiramoto Y, ShioyamaW,Kuroda T, et al. Effect of bosentan on plasma endothelin-1 concentration in patients with pulmonary arterial hypertension. Circ J 2007 Mar; 71 (3): 367-369
23. Yuyama H, Noguchi Y, Fujimori A, et al. Superiority of YM598 over atrasentan as a selective endothelin ETA receptor antagonist. Eur J Pharmacol 2004 Sep 13; 498 (1-3): 171-177 (Pubitemid 39208077)
24. Wu-Wong JR, Dixon DB, Chiou WJ, et al. Endothelin receptor antagonists: effect of serum albumin on potency and comparison of pharmacological characteristics. J Pharmacol Exp Ther 1997 May; 281 (2): 791-798
25. Yang Z, Krasnici N, Lü scher TF. Endothelin-1 potentiates human smoothmuscle cell growth to PDGF: effects of ET(A) and ET(B) receptor blockade. Circulation 1999 Jul 6; 100 (1): 5-8
26. Kunichika N, Landsberg JW, Yu Y, et al. Bosentan inhibits transient receptor potential channel expression in pulmonary vascular myocytes. Am J Respir Crit Care Med 2004 Nov 15; 170 (10): 1101-1107
27. Hettema ME, Zhang D, Stienstra Y, et al. No effects of bosentan on microvasculature in patients with limited cutaneous systemic sclerosis. Clin Rheumatol 2009 Jul; 28 (7): 825-833
28. BadeschDB, Bodin F, ChannickRN, et al. Complete results of the first randomized, placebo-controlled study of bosentan, a dual endothelin receptor antagonist, in pulmonary arterial hypertension. Curr Ther Res 2002 Apr; 63 (4): 227-246
29. Sasayama S, Kunieda T, Tomoike H, et al. Effects of the endothelin receptor antagonist bosentan on hemodynamics, symptoms and functional capacity in Japanese patients with severe pulmonary hypertension [published erratumappears in: Circ J 2005 Aug; 69 (8): 1007].
30. Circ J 2005 Feb; 69 (2): 131-137
31. Galie N, Rubin LJ, 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 Jun 21; 371 (9630): 2093-2100
32. 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 Apr; 73 (4): 372-382
33. Sauvageau S, Thorin E, Villeneuve L, et al. Change in pharmacological effect of endothelin receptor antagonists in rats with pulmonary hypertension: role ofETB-receptor expression levels. Pulm Pharmacol Ther 2009 Aug; 22 (4): 311-317
34. Mouchaers KT, Schalij I, Versteilen AMG, et al. Endothelin receptor blockade combined with phosphodiesterase-5 inhibition increases right ventricular mitochondrial capacity in pulmonary arterial hypertension. Am J Physiol Heart Circ Physiol 2009 Jul; 297 (1): H200-H207
35. European Medicines Agency. Tracleer: updated scientific discussion (tracleer-H-401-II-37-AR ) [online]. Available from URL: http://www.emea.europa. eu/humandocs/Humans/ EPAR/tracleer/tracleerM2.htm [Accessed 2009 Aug 6]
36. Cella G, Vianello F, Cozzi F, et al. Effect of bosentan on plasma markers of endothelial cell activity in patients with secondary pulmonary hypertension related to connective tissue diseases. J Rheumatol 2009 Apr; 36 (4): 760-767
37. Iannone F, Riccardi MT, Guiducci S, et al. Bosentan regulates the expression of adhesion molecules on circulating T cells and serum soluble adhesion molecules in systemic sclerosis-associated pulmonary arterial hypertension. Ann Rheum Dis 2008 Aug; 67 (8): 1121-1126
38. Hamaguchi Y, Fujimoto M, Hasegawa M, et al. Bosentan increases serum IL-12 levels in systemic sclerosis patients with pulmonary arterial hypertension [letter]. J Dermatol Sci 2009 Jul; 55 (1): 66-67
39. Giannelli G, Iannone F, Marinosci F, et al. The effect of bosentan on matrix metalloproteinase-9 levels in patients with systemic sclerosis-induced pulmonary hypertension. Curr Med Res Opin 2005 Mar; 21 (3): 327-332
40. Giannelli G, Iannone F, Marinosci F, et al. Clinical outcomes of bosentan in pulmonary arterial hypertension do not correlate with levels ofTIMPs.Eur JClin Invest 2006 Sep; 36 Suppl. 3: 73-77
41. Williams MH, Handler CE, Akram R, et al. Role of N-terminal brain natriuretic peptide (N-TproBNP) in scleroderma-associated pulmonary arterial hypertension. Eur Heart J 2006; 27 (12): 1485-1494
42. European Medicines Agency. Tracleer (bosentan) scientific discusssion [online]. Available from URL: http://www.emea. europa.eu/humandocs/PDFs/EPAR/ tracleer/100002en6.pdf [Accessed 2009 Aug 6]
43. Weber C, Gasser R, Hopfgartner G. Absorption, excretion, and metabolism of the endothelin receptor antagonist bosentan in healthymale subjects. Drug MetabDispos 1999 Jul; 27 (7): 810-815
44. Dingemanse J, Schaarschmidt D, van Giersbergen PLM. Investigation of the mutual pharmacokinetic interactions between bosentan, a dual endothelin receptor antagonist, and simvastatin. Clin Pharmacokinet 2003; 42 (3): 293-301
45. Dingemanse J, Bodin F, Weidekamm E, et al. Influence of food intake and formulation on the pharmacokinetics and metabolism of bosentan, a dual endothelin receptor antagonist. J Clin Pharmacol 2002 Mar; 42: 283-289 (Pubitemid 34163474)
46. Weber C, Schmitt R, Birnboeck H, et al. Multiple-dose pharmacokinetics, safety, and tolerability of bosentan, an endothelin receptor antagonist, in healthy male volunteers. J Clin Pharmacol 1999; 39: 703-714
47. 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 Aug; 60: 124-137
48. van Giersbergen PL, Popescu G, Bodin F, et al. Influence of mild liver impairment on the pharmacokinetics and metabolism of bosentan, a dual endothelin receptor antagonist. J Clin Pharmacol 2003 Jan; 43 (1): 15-22
49. Dingemanse J, van Giersbergen PLM. Influence of severe renal dysfunction on the pharmacokinetics and metabolism of bosentan, a dual endothelin receptor antagonist. Int J Clin Pharmacol Ther 2002 Jul; 40 (7): 310-316 (Pubitemid 34732808)
50. Binet I, Wallnö fer A, Weber C, et al. Renal hemodynamics and pharmacokinetics of bosentan with and without cyclosporine A. Kidney Int 2000 Jan; 57 (1): 224-231
51. van Giersbergen PLM, Treiber A, Clozel M, et al. In vivo and in vitro studies exploring the pharmacokinetic interaction between bosentan, a dual endothelin receptor antagonist, and glyburide. Clin Pharmacol Ther 2002; 71: 253-262
52. van Giersbergen PLM, Halabi A, Dingemanse J. Single- and multiple-dose pharmacokinetics of bosentan and its interaction with ketoconazole. Br J Clin Pharmacol 2002; 53: 589-595
53. Weber C, Banken L, Birnboeck H, et al. Effect of endothelinreceptor antagonist bosentan on the pharmacokinetics and pharmacodynamics of warfarin. J Clin Pharmacol 1999 Aug; 39 (8): 847-854
54. Weber C, Banken L, Birnboeck H, et al. The effect of bosentan on the pharmacokinetics of digoxin in healthy male subjects. Br J Clin Pharmacol 1999 Jun; 47: 701-706
55. Paul GA, Gibbs JS, Boobis AR, et al. Bosentan decreases the plasma concentration of sildenafil when coprescribed in pulmonary hypertension. Br J Clin Pharmacol 2005; 60 (1): 107-112
56. van Giersbergen PLM, Halabi A, Dingemanse J. Pharmacokinetic interaction between bosentan and the oral contraceptives norethisterone and ethinyl estradiol. Int J Clin Pharmacol Ther 2006 Mar; 44 (3): 113-118
57. van Giersbergen PL, Treiber A, Schneiter R, et al. Inhibitory and inductive effects of rifampin on the pharmacokinetics of bosentan in healthy subjects. Clin Pharmacol Ther 2007 Mar; 81 (3): 414-419
58. Burgess G, Hoogkamer H, Collings L, et al. Mutual pharmacokinetic interactions between steady-state bosentan and sildenafil. Eur J Clin Pharmacol 2008 Jan; 64 (1): 43-50
59. Treiber A, Schneiter R, Hä usler S, et al. 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 Aug; 35 (8): 1400-1407
60. Korn JH,MayesM,Matucci Cerinic M, et al. Digital ulcers in systemic sclerosis: prevention by treatment with bosentan, an oral endothelin receptor antagonist. Arthritis Rheum 2004 Dec 1; 50 (12): 3985-3993
61. Seibold JR,Matucci-Cerinic M, Denton CP, et al. Bosentan reduces the number of new digital ulcers in patients with systemic sclerosis [abstract no. OPO119]. Ann Rheum Dis 2006 Jul 1; 65 Suppl. II: 90
62. Black C, Denton CP, Furst DE, et al. Bosentan reduces the number of new digital ulcers in patients with systemic sclerosis: open label extension to a double-blind trial [abstract no. FRI0325 plus poster]. Ann Rheum Dis 2006 Jul 1; 65 Suppl. II: 384
63. Eueopean Medicines Agency. Tracleer: updated scientific discussion (tracleer-H-401-II-29-AR) [online]. Available from URL: http://www.emea.europa. eu/humandocs/PDFs/EPAR/ tracleer/EMEA-H-401-II-29-AR.pdf [Accessed 2009 Aug 6]
64. Garcia de la Peña-Lefebvre P, Rodriguez Rubio S, Valero Exposito M, et al. Long-term experience of bosentan for treating ulcers and healed ulcers in systemic sclerosis patients. Rheumatology (Oxford) 2008 Apr; 47 (4): 464-466
65. Tsifetaki N, Botzoris V, Alamanos Y, et al. Bosentan for digital ulcers in patients with systemic sclerosis: a prospective 3-year followup study [letter]. J Rheumatol 2009 Jul; 36 (7): 1550-1552
66. Humbert M, Segal ES, Kiely DG, et al. Results of European post-marketing surveillance of bosentan in pulmonary hypertension. Eur Respir J 2007 Aug; 30 (2): 338-344
67. Beghetti M, Hoeper MM, Kiely DG, et al. Safety experience with bosentan in 146 children 2-11 years old with pulmonary arterial hypertension: results from the European Postmarketing Surveillance program. Pediatr Res 2008 Aug; 64 (2): 200-204
68. Nihtyanova SI, Brough GM, Black CM, et al. Clinical burden of digital vasculopathy in limited and diffuse cutaneous systemic sclerosis. Ann Rheum Dis 2008 Jan; 67 (1): 120-123
69. Pope JE. The diagnosis and treatment of Raynaud's phenomenon: a practical approach. Drugs 2007; 67 (4): 517-525
70. Moore SC, Desantis ER. Treatment of complications associated with systemic sclerosis. Am J Health Syst Pharm 2008 Feb 15; 65 (4): 315-321
71. Kowal-Bielecka O, Landewe R, Avouac J, et al. EULAR recommendations for the treatment of systemic sclerosis: a report from the EULAR Scleroderma Trials and Research group (EUSTAR). Ann Rheum Dis 2009 May; 68 (5): 620-628
72. Gore J, SilverR. Oral sildenafil for the treatment of Raynaud's phenomenon and digital ulcers secondary to systemic sclerosis [letter]. Ann Rheum Dis 2005 Sep; 64 (9): 1387