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Chemical Compound Review

efegatran     (2S)-N-[(2S)-5- (diaminomethylideneamino)- 1...

Synonyms: CHEMBL273196, GYKI-14766, CHEBI:534837, GYKI 14766, LS-171983, ...
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Disease relevance of LY 294468

  • Minor bleeding and thrombophlebitis occurred more frequently in the efegatran treated patients [1].
  • Anticoagulant properties, clinical efficacy and safety of efegatran, a direct thrombin inhibitor, in patients with unstable angina [1].
  • Both trials evaluated efegatran combined with thrombolysis for treating acute ST-segment elevation myocardial infarction (STEMI) [2].
  • Efegatran was synthesized by the Hungarian Institute for Drug Research (IDR), which conducted phase II trials for angina in Hungary, and phase II trials for thrombosis in collaboration with Lilly in the US [182552] [3].

High impact information on LY 294468


Biological context of LY 294468

  • The thrombin time (TT) assay was prolonged twofold with 33 nM Efegatran, which demonstrated an apparent Kass value of 0.8 x 10(8) L/mol (for comparison, 17 nM hirudin was required to prolong the TT assay two-fold) [6].
  • The data suggest that LY287045, LY294291, and Efegatran should be expected to be useful as antithrombotic adjuncts to thrombolytic therapy with t-PA, urokinase, or streptokinase and should be expected to spare endogenous fibrinolysis [6].

Associations of LY 294468 with other chemical compounds


Gene context of LY 294468

  • Increase in VE-cadherin-positive cells was inhibited by hirudin and efegatran [8].
  • Outlined are the main projects and the most significant results, which include the first synthesis of human ACTH, the discovery of GYKI-14 166, the prototype of peptide inhibitors of thrombin, a stable anticoagulant, efegatran GYKI-14 766, and their dual acting analogues [9].

Analytical, diagnostic and therapeutic context of LY 294468


  1. Anticoagulant properties, clinical efficacy and safety of efegatran, a direct thrombin inhibitor, in patients with unstable angina. Klootwijk, P., Lenderink, T., Meij, S., Boersma, H., Melkert, R., Umans, V.A., Stibbe, J., Müller, E.J., Poortermans, K.J., Deckers, J.W., Simoons, M.L. Eur. Heart J. (1999) [Pubmed]
  2. Enzyme estimates of infarct size correlate with functional and clinical outcomes in the setting of ST-segment elevation myocardial infarction. Turer, A.T., Mahaffey, K.W., Gallup, D., Weaver, W.D., Christenson, R.H., Every, N.R., Ohman, E.M. Current controlled trials in cardiovascular medicine. (2005) [Pubmed]
  3. Efegatran. Institute for drug research/IVAX. Lijnen, H.R. IDrugs : the investigational drugs journal. (2001) [Pubmed]
  4. Antithrombotic assessment of the effects of combination therapy with the anticoagulants efegatran and heparin and the glycoprotein IIb-IIIa platelet receptor antagonist 7E3 in a canine model of coronary artery thrombosis. Shetler, T.J., Crowe, V.G., Bailey, B.D., Jackson, C.V. Circulation (1996) [Pubmed]
  5. Efegatran sulfate as an adjunct to streptokinase versus heparin as an adjunct to tissue plasminogen activator in patients with acute myocardial infarction. ESCALAT Investigators. Fung, A.Y., Lorch, G., Cambier, P.A., Hansen, D., Titus, B.G., Martin, J.S., Lee, J.J., Every, N.R., Hallstrom, A.P., Stock-Novack, D., Scherer, J., Weaver, W.D. Am. Heart J. (1999) [Pubmed]
  6. A family of arginal thrombin inhibitors related to efegatran. Smith, G.F., Shuman, R.T., Craft, T.J., Gifford, D.S., Kurz, K.D., Jones, N.D., Chirgadze, N., Hermann, R.B., Coffman, W.J., Sandusky, G.E., Roberts, E., Jackson, C.V. Semin. Thromb. Hemost. (1996) [Pubmed]
  7. The mechanism of binding of low-molecular-weight active site inhibitors to human alpha-thrombin. Nilsson, T., Sjöling-Ericksson, A., Deinum, J. J. Enzym. Inhib. (1998) [Pubmed]
  8. Thrombin and PAR-1 stimulate differentiation of bone marrow-derived endothelial progenitor cells. Tarzami, S.T., Wang, G., Li, W., Green, L., Singh, J.P. J. Thromb. Haemost. (2006) [Pubmed]
  9. Josef Rudinger Memorial Lecture 2002. Peptide related drug research. Bajusz, S. J. Pept. Sci. (2003) [Pubmed]
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