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Chemical Compound Review

MMTQAP     (2R,4R)-1-[(2S)-5- (diaminomethylideneamino...

Synonyms: argatroban, Argatrobanum, MPQA, MQI-ARG-MCP, CHEMBL1166, ...
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Disease relevance of argatroban

  • The combination of aspirin and argatroban may prove to be an effective therapeutic strategy in the prevention of coronary thrombosis [1].
  • We describe our experience with argatroban, a direct thrombin inhibitor, in patients with HIT or HIT with thrombosis (HITTS) [2].
  • Treatment with a direct thrombin inhibitor, such as lepirudin or argatroban, is an effective strategy in reversing the thrombocytopenia associated with HIT and reducing its complications [3].
  • OBJECTIVES: This study examined the effect of a small-molecule, direct thrombin inhibitor, argatroban, on reperfusion induced by tissue plasminogen activator (TPA) in patients with acute myocardial infarction (AMI) [4].
  • In the systemic high dose group (n = 10), angiographic thrombotic stenosis was < 5% after high dose drug delivery (p < 0.05 vs. control segments, 37.4% for heparin, 43% for argatroban) [5].

High impact information on argatroban


Chemical compound and disease context of argatroban


Biological context of argatroban

  • Patency of femoral arterial segments was maintained after the end of the intra-arterial heparin and intravenous or intra-arterial argatroban infusion for up to 3 hours despite normalization of the thrombin time and partial thromboplastin time [13].
  • Analysis of the argatroban dose-response data with a competitive inhibition model has yielded IC50 values in the low micromolar range [14].
  • This study demonstrates the differential effects of DX-9065a and argatroban on thrombin generation, which in turn results in a differential acceleration of fibrinolysis as well as TAFI activation in the clots formed under the influence of these compounds [15].
  • Platelet counts recovered more rapidly in argatroban-treated patients than in controls [2].
  • We show that clot-associated thrombin induces platelet aggregation, is resistant to heparin:antithrombin III, less so to recombinant hirudin (rHV2Lys47) but not to argatroban, an active-site directed thrombin inhibitor [16].

Anatomical context of argatroban


Associations of argatroban with other chemical compounds


Gene context of argatroban

  • Enhancement of endogenous plasminogen activator-induced thrombolysis by argatroban and APC and its control by TAFI, measured in an arterial thrombolysis model in vivo using rat mesenteric arterioles [26].
  • Argatroban, a direct thrombin inhibitor, is metabolized in vitro by CYP3A4/5 and therefore may be susceptible to clinically relevant CYP3A drug interactions [27].
  • Thrombin-induced FN secretin was also inhibited by thrombin inhibitors, such as antithrombin III, hirudin and argatroban [28].
  • Here, it appears that argatroban may be effective in controlling disorders linked to thrombin-induced VEGF production in neuronal cells [29].
  • PKSI-527, anti uPA and anti tPA IgGs suppressed argatroban-induced thrombolysis [24].

Analytical, diagnostic and therapeutic context of argatroban

  • Scanning electron microscopy/morphometric analyses demonstrated that permeation with argatroban had no significant effects on clot structure [14].
  • The antithrombotic activity of argatroban has been quantified in fibrin clot permeation and fibrin clot perfusion systems as a function of clot age and composition [14].
  • CONCLUSIONS: Argatroban, as compared with heparin, appears to enhance reperfusion with TPA in patients with AMI, particularly in those patients with delayed presentation [4].
  • The slope depended on the argatroban dose and on the International Sensitivity Index (ISI) of the PT reagent, the steepest slope (i.e., the largest difference between INR (ARG+VKA) and INR (VKA alone)) was seen with the highest ARG dose and the PT reagent with an ISI of 2.13 [30].
  • Systemic argatroban clearance increased approximately 20% during hemodialysis, without clinically significantly affecting ACTs [17].


  1. Combined administration of aspirin and a specific thrombin inhibitor in man. Clarke, R.J., Mayo, G., FitzGerald, G.A., Fitzgerald, D.J. Circulation (1991) [Pubmed]
  2. Argatroban anticoagulation in patients with heparin-induced thrombocytopenia. Lewis, B.E., Wallis, D.E., Leya, F., Hursting, M.J., Kelton, J.G. Arch. Intern. Med. (2003) [Pubmed]
  3. Heparin-induced thrombocytopenia: clinical manifestations and management strategies. Menajovsky, L.B. Am. J. Med. (2005) [Pubmed]
  4. A multicenter, randomized study of argatroban versus heparin as adjunct to tissue plasminogen activator (TPA) in acute myocardial infarction: myocardial infarction with novastan and TPA (MINT) study. Jang, I.K., Brown, D.F., Giugliano, R.P., Anderson, H.V., Losordo, D., Nicolau, J.C., Dutra, O.P., Bazzino, O., Viamonte, V.M., Norbady, R., Liprandi, A.S., Massey, T.J., Dinsmore, R., Schwarz, R.P. J. Am. Coll. Cardiol. (1999) [Pubmed]
  5. Local treatment with antithrombotic drugs can prevent thrombus formation: an angioscopic and angiographic study. Tomaru, T., Nakamura, F., Fujimori, Y., Omata, M., Kawai, S., Okada, R., Murata, Y., Uchida, Y. J. Am. Coll. Cardiol. (1995) [Pubmed]
  6. Platelet activation with unfractionated heparin at therapeutic concentrations and comparisons with a low-molecular-weight heparin and with a direct thrombin inhibitor. Xiao, Z., Théroux, P. Circulation (1998) [Pubmed]
  7. Role of thrombin and thromboxane A2 in reocclusion following coronary thrombolysis with tissue-type plasminogen activator. Fitzgerald, D.J., Fitzgerald, G.A. Proc. Natl. Acad. Sci. U.S.A. (1989) [Pubmed]
  8. Antithrombotic and hemorrhagic effects of DX-9065a, a direct and selective factor Xa inhibitor: comparison with a direct thrombin inhibitor and antithrombin III-dependent anticoagulants. Morishima, Y., Tanabe, K., Terada, Y., Hara, T., Kunitada, S. Thromb. Haemost. (1997) [Pubmed]
  9. Laboratory tests for heparin-induced thrombocytopenia: a multicenter study. Walenga, J.M., Jeske, W.P., Wood, J.J., Ahmad, S., Lewis, B.E., Bakhos, M. Semin. Hematol. (1999) [Pubmed]
  10. Antithrombotic effects of FK419, a novel nonpeptide platelet GPIIb/IIIa antagonist, in a guinea pig photochemically induced middle cerebral artery thrombosis model: comparison with ozagrel and argatroban. Moriguchi, A., Aoki, T., Mihara, K., Tojo, N., Matsuoka, N., Mutoh, S. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
  11. Transitioning from argatroban to warfarin therapy in patients with heparin-induced thrombocytopenia. Hursting, M.J., Lewis, B.E., Macfarlane, D.E. Clin. Appl. Thromb. Hemost. (2005) [Pubmed]
  12. Synergistic antithrombotic effects of argatroban and ticlopidine in the rat venous thrombosis model. Morishita, K., Iwamoto, M. Thromb. Res. (1998) [Pubmed]
  13. Prevention of platelet-rich arterial thrombosis by selective thrombin inhibition. Jang, I.K., Gold, H.K., Ziskind, A.A., Leinbach, R.C., Fallon, J.T., Collen, D. Circulation (1990) [Pubmed]
  14. No effect of clot age or thrombolysis on argatroban's inhibition of thrombin. Hantgan, R.R., Jerome, W.G., Hursting, M.J. Blood (1998) [Pubmed]
  15. Studies on the different modes of action of the anticoagulant protease inhibitors DX-9065a and Argatroban. II. Effects on fibrinolysis. Nagashima, H. J. Biol. Chem. (2002) [Pubmed]
  16. Inhibition by Argatroban, a specific thrombin inhibitor, of platelet activation by fibrin clot-associated thrombin. Lunven, C., Gauffeny, C., Lecoffre, C., O'Brien, D.P., Roome, N.O., Berry, C.N. Thromb. Haemost. (1996) [Pubmed]
  17. A prospective comparison of three argatroban treatment regimens during hemodialysis in end-stage renal disease. Murray, P.T., Reddy, B.V., Grossman, E.J., Hammes, M.S., Trevino, S., Ferrell, J., Tang, I., Hursting, M.J., Shamp, T.R., Swan, S.K. Kidney Int. (2004) [Pubmed]
  18. Synergistic antithrombotic properties of G4120, a RGD-containing synthetic peptide, and argatroban, a synthetic thrombin inhibitor, in a hamster femoral vein platelet-rich thrombosis model. Imura, Y., Stassen, J.M., Vreys, I., Lesaffre, E., Gold, H.K., Collen, D. Thromb. Haemost. (1992) [Pubmed]
  19. Thrombin inhibitor reduces leukocyte-endothelial cell interactions and vascular leakage after scatter laser photocoagulation. Musashi, K., Kiryu, J., Miyamoto, K., Miyahara, S., Katsuta, H., Tamura, H., Hirose, F., Yoshimura, N. Invest. Ophthalmol. Vis. Sci. (2005) [Pubmed]
  20. Effects of a thrombin inhibitor, argatroban, on ischemic brain damage in the rat distal middle cerebral artery occlusion model. Kawai, H., Yuki, S., Sugimoto, J., Tamao, Y. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  21. Small, noncovalent serine protease inhibitors. Sanderson, P.E. Medicinal research reviews. (1999) [Pubmed]
  22. Interpreting the International Normalized Ratio (INR) in individuals receiving argatroban and warfarin. Sheth, S.B., DiCicco, R.A., Hursting, M.J., Montague, T., Jorkasky, D.K. Thromb. Haemost. (2001) [Pubmed]
  23. Differences in the clinically effective molar concentrations of four direct thrombin inhibitors explain their variable prothrombin time prolongation. Warkentin, T.E., Greinacher, A., Craven, S., Dewar, L., Sheppard, J.A., Ofosu, F.A. Thromb. Haemost. (2005) [Pubmed]
  24. Suppression of argatroban-induced endogenous thrombolysis by PKSI-527, and antibodies to TPA and UPA, evaluated in a rat arterial thrombolysis model. Hashimoto, M., Oiwa, K., Matsuo, O., Ueshima, S., Okada, K., Okada, Y., Okamoto, S., Giddings, J.C., Yamamoto, J. Thromb. Haemost. (2003) [Pubmed]
  25. Antithrombotic effects of TAK-029, a novel GPIIb/IIIa antagonist, in guinea pigs: comparative studies with ticlopidine, clopidogrel, aspirin, prostaglandin E1 and argatroban. Kawamura, M., Imura, Y., Moriya, N., Kita, S., Fukushi, H., Sugihara, H., Nishikawa, K., Terashita, Z. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  26. Enhancement of endogenous plasminogen activator-induced thrombolysis by argatroban and APC and its control by TAFI, measured in an arterial thrombolysis model in vivo using rat mesenteric arterioles. Hashimoto, M., Yamashita, T., Oiwa, K., Watanabe, S., Giddings, J.C., Yamamoto, J. Thromb. Haemost. (2002) [Pubmed]
  27. Assessment of the potential pharmacokinetic and pharmacodynamic interactions between erythromycin and argatroban. Tran, J.Q., Di Cicco, R.A., Sheth, S.B., Tucci, M., Peng, L., Jorkasky, D.K., Hursting, M.J., Benincosa, L.J. Journal of clinical pharmacology. (1999) [Pubmed]
  28. Thrombin stimulates production of fibronectin by human proximal tubular epithelial cells via a transforming growth factor-beta-dependent mechanism. Shirato, K., Osawa, H., Kaizuka, M., Nakamura, N., Sugawara, T., Nakamura, M., Tamura, M., Yamabe, H., Okumura, K. Nephrol. Dial. Transplant. (2003) [Pubmed]
  29. Inhibition of thrombin-induced vascular endothelial growth factor production in human neuroblastoma (NB-1) cells by argatroban. Sarker, K.P., Biswas, K.K., Yamaji, K., Yamakuchi, M., Hashiguchi, T., Lee, K.Y., Maruyama, I. Pathophysiol. Haemost. Thromb. (2005) [Pubmed]
  30. Transition from argatroban to oral anticoagulation with phenprocoumon or acenocoumarol: effects on prothrombin time, activated partial thromboplastin time, and Ecarin Clotting Time. Harder, S., Graff, J., Klinkhardt, U., von Hentig, N., Walenga, J.M., Watanabe, H., Osakabe, M., Breddin, H.K. Thromb. Haemost. (2004) [Pubmed]
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