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Chemical Compound Review

Tezosentan     N-[6-(2-hydroxyethoxy)-5-(2...

Synonyms: SureCN4524, SureCN4525, CHEMBL61780, CHEBI:194071, KB-81086, ...
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Disease relevance of Tezosentan

  • Adverse events, more frequent with tezosentan than with placebo (headache, asymptomatic hypotension, early worsening of renal function, nausea, vomiting), were dose-related [1].
  • OBJECTIVES: The objective of this study was to evaluate the addition of intravenous (IV) tezosentan to standard therapy for patients with pulmonary edema [2].
  • BACKGROUND: Tezosentan is an IV nonselective endothelin (ET)-1 antagonist that yields favorable hemodynamic effects in patients with acute congestive heart failure (CHF) [2].
  • A tendency for an improved dyspnea score and a decreased risk of clinical worsening was observed after 24 h of treatment with each tezosentan dose [1].
  • METHODS: Rats with cirrhosis received LPS and then tezosentan or placebo one hour later [3].

High impact information on Tezosentan

  • Tezosentan, an endothelin receptor antagonist, limits liver injury in endotoxin challenged cirrhotic rats [3].
  • Tezosentan significantly decreased hepatic MPO activity and hepatic neutrophils but had no effect on LPS induced iNOS or COX-2 [3].
  • Plasma TNF-alpha levels were significantly lower in rats receiving LPS and tezosentan (182 (38) pg/ml) compared with those receiving LPS alone (821 (212) pg/ml) [3].
  • The aim of this study was to investigate the effects of tezosentan, a non-selective ETA and ETB receptor antagonist, in LPS challenged rats with cirrhosis [3].
  • OBJECTIVES: We sought to investigate the efficacy and safety of tezosentan, a dual endothelin receptor antagonist, in patients hospitalized for acute heart failure (HF) [1].

Chemical compound and disease context of Tezosentan


Biological context of Tezosentan


Anatomical context of Tezosentan


Associations of Tezosentan with other chemical compounds


Gene context of Tezosentan

  • Tezosentan (10(-4) mol/l) blocked the ET-1-induced response in human and possum GB strips (p<0.001) [22].
  • The lower dose of tezosentan also produced a decrease in the endothelin-3-induced gallbladder pressure (P < 0.02) but not in blood pressure, whereas the higher dose reduced the blood pressure with no further reduction in gallbladder pressure (P < 0.05) [23].
  • Administration of EDN2 to the ovarian tissue induced rapid contraction, whereas addition of tezosentan, an endothelin receptor antagonist, diminishes the EDN2 effect [12].
  • Tezosentan competitively antagonizes the specific binding of (125)I-labeled ET-1 and of the selective ET(B) receptor ligands (125)I-labeled ET-3 and (125)I-labeled sarafotoxin S6c on cells and tissues carrying ET(A) and ET(B) receptors, with inhibitory constants in the nanomolar range, and has high water solubility [17].
  • Tezosentan alone did not have any effect on haemodynamics, plasma levels of NO(2)(-)/NO(3)(-) or iNOS activity [24].

Analytical, diagnostic and therapeutic context of Tezosentan

  • Three groups were studied: I/R untreated (n=17), I/R pretreated (n=11), and I/R posttreated (n=13) with Tezosentan (15 mg/kg, i.v.). RESULTS: Tezosentan significantly decreased (P<0.05) the rise in Scr from I/R injury (2.0+/-0.4 mg/dl, before and 2.9+/-0.4 mg/dl, after treatment) compared with untreated animals (4.2+/-0.4 mg/dl) [25].
  • All animals treated with tezosentan survived, whereas in the control group four out of six animals died [14].
  • In addition, four healthy sheep, exposed to an intravenous infusion of endothelin-1 at 20 ng x kg x min, after 1 hr received tezosentan in stepwise increasing doses of 0.5, 1, and 2 mg x kg x hr that were maintained for 1 hr each [15].
  • Tezosentan treatment did not produce any alterations in hepatocellular injury or hepatic redox status when compared with the untreated animals receiving 6 hrs of ischemia/reperfusion [16].
  • However, the effect was not sustained with higher doses of tezosentan, possibly due to reduced coronary perfusion pressure [26].


  1. Hemodynamic and clinical effects of tezosentan, an intravenous dual endothelin receptor antagonist, in patients hospitalized for acute decompensated heart failure. Torre-Amione, G., Young, J.B., Colucci, W.S., Lewis, B.S., Pratt, C., Cotter, G., Stangl, K., Elkayam, U., Teerlink, J.R., Frey, A., Rainisio, M., Kobrin, I. J. Am. Coll. Cardiol. (2003) [Pubmed]
  2. RITZ-5: randomized intravenous TeZosentan (an endothelin-A/B antagonist) for the treatment of pulmonary edema: a prospective, multicenter, double-blind, placebo-controlled study. Kaluski, E., Kobrin, I., Zimlichman, R., Marmor, A., Krakov, O., Milo, O., Frey, A., Kaplan, S., Krakover, R., Caspi, A., Vered, Z., Cotter, G. J. Am. Coll. Cardiol. (2003) [Pubmed]
  3. Tezosentan, an endothelin receptor antagonist, limits liver injury in endotoxin challenged cirrhotic rats. Urbanowicz, W., Sogni, P., Moreau, R., Tazi, K.A., Barriere, E., Poirel, O., Martin, A., Guimont, M.C., Cazals-Hatem, D., Lebrec, D. Gut (2004) [Pubmed]
  4. Role of endothelin-1 and thromboxane A2 in the pulmonary hypertension induced by heparin-protamine interaction in anesthetized dogs. Freitas, C.F., Faro, R., Dragosavac, D., Clozel, M., De Nucci, G., Antunes, E. J. Cardiovasc. Pharmacol. (2004) [Pubmed]
  5. Nebulized therapies for childhood pulmonary hypertension: an in vitro model. Katz, S.L., Adatia, I., Louca, E., Leung, K., Humpl, T., Reyes, J.T., Coates, A.L. Pediatr. Pulmonol. (2006) [Pubmed]
  6. Current status of endothelin blockade for the treatment of cardiovascular and pulmonary vascular disease. Krum, H., Liew, D. Current opinion in investigational drugs (London, England : 2000) (2003) [Pubmed]
  7. Tezosentan, a combined parenteral endothelin receptor antagonist, produces pulmonary vasodilation in lambs with acute and chronic pulmonary hypertension. Fitzgerald, R.K., Oishi, P., Ovadia, B., Ross, G.A., Reinhartz, O., Johengen, M.J., Fineman, J.R. Pediatric critical care medicine : a journal of the Society of Critical Care Medicine and the World Federation of Pediatric Intensive and Critical Care Societies. (2004) [Pubmed]
  8. Endothelin receptor blockade improves oxygenation in contralateral TRAM flap tissue in pigs. Erni, D., Wessendorf, R., Wettstein, R., Schilling, M.K., Banic, A. British journal of plastic surgery. (2001) [Pubmed]
  9. Tezosentan in patients with acute heart failure and acute coronary syndromes: results of the Randomized Intravenous TeZosentan Study (RITZ-4). O'Connor, C.M., Gattis, W.A., Adams, K.F., Hasselblad, V., Chandler, B., Frey, A., Kobrin, I., Rainisio, M., Shah, M.R., Teerlink, J., Gheorghiade, M. J. Am. Coll. Cardiol. (2003) [Pubmed]
  10. Active endothelin is an important vasoconstrictor in acute coronary thrombi. Adlbrecht, C., Bonderman, D., Plass, C., Jakowitsch, J., Beran, G., Sperker, W., Siostrzonek, P., Glogar, D., Maurer, G., Lang, I.M. Thromb. Haemost. (2007) [Pubmed]
  11. Contribution of endothelin and its receptors to the regulation of vascular tone during exercise is different in the systemic, coronary and pulmonary circulation. Merkus, D., Houweling, B., Mirza, A., Boomsma, F., van den Meiracker, A.H., Duncker, D.J. Cardiovasc. Res. (2003) [Pubmed]
  12. Endothelin-2 in ovarian follicle rupture. Ko, C., Gieske, M.C., Al-Alem, L., Hahn, Y., Su, W., Gong, M.C., Iglarz, M., Koo, Y. Endocrinology (2006) [Pubmed]
  13. Short-term endothelin receptor blockade with tezosentan has both immediate and long-term beneficial effects in rats with myocardial infarction. Clozel, M., Qiu, C., Qiu, C.S., Hess, P., Clozel, J.P. J. Am. Coll. Cardiol. (2002) [Pubmed]
  14. Tezosentan decreases pulmonary artery pressure and improves survival rate in an animal model of meconium aspiration. Geiger, R., Pajk, W., Neu, N., Maier, S., Kleinsasser, A., Fratz, S., Navarro-Psiha, S., Fischer, V., Treml, B., Loeckinger, A. Pediatr. Res. (2006) [Pubmed]
  15. Novel endothelin receptor antagonist attenuates endotoxin-induced lung injury in sheep. Kuklin, V.N., Kirov, M.Y., Evgenov, O.V., Sovershaev, M.A., Sjöberg, J., Kirova, S.S., Bjertnaes, L.J. Crit. Care Med. (2004) [Pubmed]
  16. Carbon monoxide, but not endothelin-1, plays a major role for the hepatic microcirculation in a murine model of early systemic inflammation. Wunder, C., Brock, R.W., Frantz, S., Göttsch, W., Morawietz, H., Roewer, N., Eichelbrönner, O. Crit. Care Med. (2005) [Pubmed]
  17. Pharmacology of tezosentan, new endothelin receptor antagonist designed for parenteral use. Clozel, M., Ramuz, H., Clozel, J.P., Breu, V., Hess, P., Löffler, B.M., Coassolo, P., Roux, S. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  18. Role of endothelin in alpha-adrenoceptor coronary vasoconstriction. Gorman, M.W., Farias, M., Richmond, K.N., Tune, J.D., Feigl, E.O. Am. J. Physiol. Heart Circ. Physiol. (2005) [Pubmed]
  19. Preconditioning protects endothelium by preventing ET-1-induced activation of NADPH oxidase and xanthine oxidase in post-ischemic heart. Duda, M., Konior, A., Klemenska, E., Beresewicz, A. J. Mol. Cell. Cardiol. (2007) [Pubmed]
  20. Effects of a dual endothelin-1 receptor antagonist on airway obstruction and acute lung injury in sheep following smoke inhalation and burn injury. Cox, R.A., Enkhabaatar, P., Burke, A.S., Katahira, J., Shimoda, K., Chandra, A., Traber, L.D., Herndon, D.N., Hawkins, H.K., Traber, D.L. Clin. Sci. (2005) [Pubmed]
  21. Influence of dual ET(A)/ET(B)-receptor blockade on coronary responses to treadmill exercise in dogs. Takamura, M., Parent, R., Cernacek, P., Lavallée, M. J. Appl. Physiol. (2000) [Pubmed]
  22. Endothelin-1 induces contraction of human and Australian possum gallbladder in vitro. Al-Jiffry, B.O., Meedeniya, A.C., Chen, J.W., Toouli, J., Saccone, G.T. Regul. Pept. (2001) [Pubmed]
  23. Endothelins induce gallbladder contraction independent of elevated blood pressure in vivo in the Australian possum. Al-Jiffry, B.O., Chen, J.W., Toouli, J., Saccone, G.T. J. Gastrointest. Surg. (2002) [Pubmed]
  24. Haemodynamic effects of endothelin receptor antagonist, tezosentan, in tumour necrosis factor-alpha treated anaesthetized rats. Tabrizchi, R., Ford, C.A. Naunyn Schmiedebergs Arch. Pharmacol. (2003) [Pubmed]
  25. The use of the endothelin receptor antagonist, tezosentan, before or after renal ischemia protects renal function. Wilhelm, S.M., Stowe, N.T., Robinson, A.V., Schulak, J.A. Transplantation (2001) [Pubmed]
  26. Differentiated and dose-related cardiovascular effects of a dual endothelin receptor antagonist in endotoxin shock. Konrad, D., Oldner, A., Rossi, P., Wanecek, M., Rudehill, A., Weitzberg, E. Crit. Care Med. (2004) [Pubmed]
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