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Chemical Compound Review

Ifetroban     3-[2-[[(1S,5S,6R)-5-[4- (pentylcarbamoyl)-1...

Synonyms: SureCN28136, BMS180291, BMS 180291, AC1L228B, AC1Q5P9O, ...
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Disease relevance of Ifetroban

  • Effect of aspirin and ifetroban on skeletal muscle blood flow in patients with congestive heart failure treated with Enalapril. Ifetroban Study Group [1].
  • In interaction studies, aspirin was injected i.v. 10 min prior to occlusion (10 mg/kg) and at the 45th min of ischemia (5 mg/kg) both with and without subsequent administration of ifetroban (0.3 mg/kg + 0.3 mg/kg per h) beginning at the 75th min of occlusion [2].
  • BACKGROUND: To determine the results of standardized ulcer treatment regimes and effects of the oral thromboxane A2 antagonist Ifetroban (250 mg daily) on healing of chronic lower-extremity venous stasis ulcers [3].
  • Dose-related cardioprotection by ifetroban in relation to inhibition of thrombosis and ex vivo platelet function [4].
  • These observations suggest that a mechanism involving nitric oxide and potassium channels facilitates the reduction in basal tone produced by ifetroban in aortic rings of rats with aortic coarctation-induced hypertension [5].

High impact information on Ifetroban


Biological context of Ifetroban


Anatomical context of Ifetroban

  • Rings with endothelium from normotensive rats were unaffected by indomethacin and ifetroban [9].
  • Ifetroban alone significantly (P < 0.05) reduced infarct size compared to vehicle treatment (13 +/- 1% vs. 23 +/- 2% of left ventricle), and this was not prevented by combination with aspirin (12 +/- 2% vs. 22 +/- 3% of left ventricle) [2].
  • In dogs, ifetroban (1 + 1 mg/kg/h, intravenously, i.v.) or vehicle administration was initiated 10 min before left circumflex coronary artery (LCX) occlusion [14].
  • Thus, doses of ifetroban causing profound TP receptor blockade also salvaged jeopardized myocardium in dogs and ferrets without changing collateral BF or peripheral hemodynamics [14].
  • Additional experiments in ferrets tested the antithrombotic potency of ifetroban as an inhibitor of thrombotic cyclic flow reduction (CFR) in the stenosed abdominal aorta (Folts model) [4].

Associations of Ifetroban with other chemical compounds


Gene context of Ifetroban


Analytical, diagnostic and therapeutic context of Ifetroban


  1. Effect of aspirin and ifetroban on skeletal muscle blood flow in patients with congestive heart failure treated with Enalapril. Ifetroban Study Group. Katz, S.D., Radin, M., Graves, T., Hauck, C., Block, A., LeJemtel, T.H. J. Am. Coll. Cardiol. (1999) [Pubmed]
  2. Failure of aspirin to interfere with the cardioprotective effects of ifetroban. Gomoll, A.W., Ogletree, M.L. Eur. J. Pharmacol. (1994) [Pubmed]
  3. Clinical benchmark for healing of chronic venous ulcers. Venous Ulcer Study Collaborators. Lyon, R.T., Veith, F.J., Bolton, L., Machado, F. Am. J. Surg. (1998) [Pubmed]
  4. Dose-related cardioprotection by ifetroban in relation to inhibition of thrombosis and ex vivo platelet function. Gomoll, A.W., Schumacher, W.A., Ogletree, M.L. Pharmacology (1995) [Pubmed]
  5. Involvement of nitric oxide and potassium channels in the reduction of basal tone produced by blockade of thromboxane A2/prostaglandin H2 receptors in aortic rings of hypertensive rats. DelliPizzi, A., Nasjletti, A. Clin. Exp. Hypertens. (1998) [Pubmed]
  6. Relationship between hypercholesterolaemia, endothelial dysfunction and hypertension. Hayakawa, H., Raij, L. J. Hypertens. (1999) [Pubmed]
  7. Inhibition of prostaglandin D2 clearance in rat hepatocytes by the thromboxane receptor antagonists daltroban and ifetroban and the thromboxane synthase inhibitor furegrelate. Pestel, S., Nath, A., Jungermann, K., Schieferdecker, H.L. Biochem. Pharmacol. (2003) [Pubmed]
  8. Neuropeptide Y-induced potentiation of noradrenergic vasoconstriction in the human saphenous vein: involvement of endothelium generated thromboxane. Fabi, F., Argiolas, L., Ruvolo, G., del Basso, P. Br. J. Pharmacol. (1998) [Pubmed]
  9. Contribution of constrictor prostanoids to the calcium-dependent basal tone in the aorta from rats with aortic coarctation-induced hypertension: relationship to nitric oxide. Dellipizzi, A., Pucci, M.L., Mosny, A.Y., Deseyn, K., Nasjletti, A. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  10. Direct vasoconstrictor effects of sandimmune (cyclosporine A) are mediated by its vehicle cremophor EL: inhibition by the thromboxane A2/prostaglandin endoperoxide receptor antagonist ifetroban. Lodge, N.J. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  11. Disposition of radiolabeled ifetroban in rats, dogs, monkeys, and humans. Dockens, R.C., Santone, K.S., Mitroka, J.G., Morrison, R.A., Jemal, M., Greene, D.S., Barbhaiya, R.H. Drug Metab. Dispos. (2000) [Pubmed]
  12. Effect of ifetroban, a thromboxane A2 receptor antagonist, in stroke-prone spontaneously hypertensive rats. Johnson, R.A., Belmonte, A., Fan, N.Y., Lavesa, M., Nasjletti, A., Stier, C.T. Clin. Exp. Hypertens. (1996) [Pubmed]
  13. Ifetroban sodium: an effective TxA2/PGH2 receptor antagonist. Rosenfeld, L., Grover, G.J., Stier, C.T. Cardiovascular drug reviews. (2001) [Pubmed]
  14. Myocardial salvage efficacy of the thromboxane receptor antagonist ifetroban in ferrets and dogs. Gomoll, A.W., Grover, G.J., Ogletree, M.L. J. Cardiovasc. Pharmacol. (1994) [Pubmed]
  15. Role of endothelin-1 and thromboxane A2 in renal vasoconstriction induced by angiotensin II in diabetes and hypertension. Cediel, E., Vázquez-Cruz, B., Navarro-Cid, J., De Las Heras, N., Sanz-Rosa, D., Cachofeiro, V., Lahera, V. Kidney Int. Suppl. (2002) [Pubmed]
  16. Dissociation of endothelial cell dysfunction and blood pressure in SHR. Tesfamariam, B., Ogletree, M.L. Am. J. Physiol. (1995) [Pubmed]
  17. AT1 and TxA2/PGH2 receptors maintain hypertension throughout 2K,1C Goldblatt hypertension in the rat. Wilcox, C.S., Cardozo, J., Welch, W.J. Am. J. Physiol. (1996) [Pubmed]
  18. AT-1 receptor antagonism modifies the mediation of endothelin-1, thromboxane A2, and catecholamines in the renal constrictor response to angiotensin II. Cediel, E., de Las Heras, N., Sanz-Rosa, D., Velasco, O., Cachofeiro, V., Lahera, V. Kidney Int. Suppl. (2005) [Pubmed]
  19. Intravascular thrombosis after hypoxia-induced pulmonary hypertension: regulation by cyclooxygenase-2. Pidgeon, G.P., Tamosiuniene, R., Chen, G., Leonard, I., Belton, O., Bradford, A., Fitzgerald, D.J. Circulation (2004) [Pubmed]
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