Sitaxsentan: a selective endothelin-A receptor antagonist, for the treatment of pulmonary arterial hypertension

被引:31
作者
Barst, Robyn J.
机构
[1] Columbia Univ Coll Phys & Surg, New York, NY 10032 USA
[2] New York Presbyterian Pulm Hypertens Ctr, New York, NY USA
关键词
endothelin-1; endothelin receptor antagonist; pulmonary arterial hypertension;
D O I
10.1517/14656566.8.1.95
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Pulmonary arterial hypertension (PAH) is a progressive, life-threatening condition. Sitaxsentan, a selective enclothelin-A receptor antagonist, is an effective, safe and well-tolerated enclothelin receptor antagonist for the treatment of PAH in adult patients. Multi-center, randomized, placebo-controlled clinical trials have demonstrated that sitaxsentan has beneficial effects on exercise capacity (i.e., 6-min walk distance), functional class and hemodynamic parameters in PAH patients. Sitaxsentan has a low incidence of acute hepatotoxicity. Patients on concomitant warfarin require a decrease in warfarin dose to maintain a therapeutic international normalized ratio. The demonstration of clinical efficacy and low incidence of acute hepatotoxicity support the potential use of sitaxsentan for the treatment of PAH.
引用
收藏
页码:95 / 109
页数:15
相关论文
共 49 条
[1]  
Abraham DJ, 1997, AM J PATHOL, V151, P831
[2]   Continuous intravenous epoprostenol for pulmonary hypertension due to the scleroderma spectrum of disease -: A randomized, controlled trial [J].
Badesch, DB ;
Tapson, VF ;
McGoon, MD ;
Brundage, BH ;
Rubin, LJ ;
Wigley, FM ;
Rich, S ;
Barst, RJ ;
Barrett, PS ;
Kral, KM ;
Jöbsis, MM ;
Loyd, JE ;
Murali, S ;
Frost, A ;
Girgis, R ;
Bourge, RC ;
Ralph, DD ;
Elliott, CG ;
Hill, NS ;
Langleben, D ;
Schilz, RJ ;
McLaughlin, VV ;
Robbins, IM ;
Groves, BM ;
Shapiro, S ;
Medsger, TA ;
Gaine, SP ;
Horn, E ;
Decker, JC ;
Knobil, K .
ANNALS OF INTERNAL MEDICINE, 2000, 132 (06) :425-+
[3]   Pharmacokinetics, safety, and efficacy of bosentan in pediatric patients with pulmonary arterial hypertension [J].
Barst, RJ ;
Ivy, D ;
Dingemanse, J ;
Widlitz, A ;
Schmitt, K ;
Doran, A ;
Bingaman, D ;
Nguyen, N ;
Gaitonde, M ;
van Giersbergen, PLM .
CLINICAL PHARMACOLOGY & THERAPEUTICS, 2003, 73 (04) :372-382
[4]   Sitaxsentan therapy for pulmonary arterial hypertension [J].
Barst, RJ ;
Langleben, D ;
Frost, A ;
Horn, EM ;
Oudiz, R ;
Shapiro, S ;
McLaughlin, V ;
Hill, N ;
Tapson, VF ;
Robbins, IM ;
Zwicke, D ;
Duncan, B ;
Dixon, RAF ;
Frumkin, LR .
AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE, 2004, 169 (04) :441-447
[5]   Clinical efficacy of sitaxsentan, an endothelin-A receptor antagonist, in patients with pulmonary arterial hypertension - Open-label pilot study [J].
Barst, RJ ;
Rich, S ;
Widlitz, A ;
Horn, EM ;
McLaughlin, V ;
McFarlin, J .
CHEST, 2002, 121 (06) :1860-1868
[6]   A comparison of continuous intravenous epoprostenol (prostacyclin) with conventional therapy for primary pulmonary hypertension [J].
Barst, RJ ;
Rubin, LJ ;
Long, WA ;
McGoon, MD ;
Rich, S ;
Badesch, DB ;
Groves, BM ;
Tapson, VF ;
Bourge, RC ;
Brundage, BH ;
Koerner, SK ;
Langleben, D ;
Keller, CA ;
Murali, S ;
Uretsky, BF ;
Clayton, LM ;
Jobsis, MM ;
Blackburn, SD ;
Shortino, D ;
Crow, JW .
NEW ENGLAND JOURNAL OF MEDICINE, 1996, 334 (05) :296-301
[7]   Beraprost therapy for pulmonary arterial hypertension [J].
Barst, RJ ;
McGoon, M ;
McLaughlin, V ;
Tapson, V ;
Oudiz, R ;
Shapiro, S ;
Robbins, IM ;
Channick, R ;
Badesch, D ;
Rayburn, BK ;
Flinchbaugh, R ;
Sigman, J ;
Arneson, C ;
Jeffs, R .
JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY, 2003, 41 (12) :2119-2125
[8]   Treatment of pulmonary arterial hypertension with the selective endothelin-A receptor antagonist sitaxsentan [J].
Barst, Robyn J. ;
Langleben, David ;
Badesch, David ;
Frost, Adaani ;
Lawrence, E. Clinton ;
Shapiro, Shelley ;
Naeije, Robert ;
Galie, Nazzareno .
JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY, 2006, 47 (10) :2049-2056
[9]   Selective upregulation of endothelin B receptor gene expression in severe pulmonary hypertension [J].
Bauer, M ;
Wilkens, HC ;
Langer, F ;
Schneider, SO ;
Lausberg, H ;
Schäfers, HJ .
CIRCULATION, 2002, 105 (09) :1034-1036
[10]  
BENZA RL, 2006, 26 ISHLT ANN M SCI S, P94