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Chemical Compound Review

Melagatran     2-[[(1R)-2-[(2S)-2-[(4...

Synonyms: SureCN27652, CHEMBL266349, CHEBI:43966, LS-72219, CTK8F0798, ...
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Disease relevance of Melagatran


High impact information on Melagatran

  • Overall, a significant dose-dependent decrease in VTE was seen with melagatran/ximelagatran (lowest to highest group: 111 [37.8%], 70 [24.1%], 71 [23.7%], and 43 [15.1%]; p=0.0001); there were also significant relations for both total hip and total knee replacement individually [1].
  • At concentrations from 1 to 10 micromol/l, Melagatran inhibited both coagulation and complement activation [5].
  • In this study, the hypothesis that a specific thrombin inhibitor, Melagatran, could reduce IBMIR in an in vitro model in which human islets are exposed to ABO-compatible blood was tested [5].
  • Islets exposed to blood, in the absence or presence of 0.4 micromol/l Melagatran, exhibited a loss of integrity and were found to be trapped in macroscopic clots containing platelets and CD11b(+) leukocytes [5].
  • Melagatran showed dose-proportional pharmacokinetics with low variability [6].

Chemical compound and disease context of Melagatran


Biological context of Melagatran


Anatomical context of Melagatran


Associations of Melagatran with other chemical compounds


Gene context of Melagatran


Analytical, diagnostic and therapeutic context of Melagatran

  • We did a multicentre, randomised, double-blind study to examine the dose-response relation of subcutaneous melagatran, a direct thrombin inhibitor, followed by oral ximelagatran as thromboprophylaxis after total hip or knee replacement [1].
  • Inhibition of thrombin abrogates the instant blood-mediated inflammatory reaction triggered by isolated human islets: possible application of the thrombin inhibitor melagatran in clinical islet transplantation [5].
  • CONCLUSION: There were no differences in the pharmacokinetic or pharmacodynamic properties of melagatran following oral administration of ximelagatran between the hepatically impaired and control volunteers [11].
  • RESULTS: For the volunteers with severe renal impairment, the area under the plasma concentration-time curve (AUC) and the half-life of melagatran were significantly higher than in the control group with normal renal function [25].
  • It was found that INR depends not only on the plasma concentration of melagatran, but also on the sensitivity of the PT reagent and on the final dilution of the plasma sample in the prothrombin time assay [24].


  1. Ximelagatran and melagatran compared with dalteparin for prevention of venous thromboembolism after total hip or knee replacement: the METHRO II randomised trial. Eriksson, B.I., Bergqvist, D., Kälebo, P., Dahl, O.E., Lindbratt, S., Bylock, A., Frison, L., Eriksson, U.G., Welin, L., Gustafsson, D. Lancet (2002) [Pubmed]
  2. Pharmacokinetics of ximelagatran and relationship to clinical response in acute deep vein thrombosis. Cullberg, M., Eriksson, U.G., Wåhlander, K., Eriksson, H., Schulman, S., Karlsson, M.O. Clin. Pharmacol. Ther. (2005) [Pubmed]
  3. Local proCPU (TAFI) activation during thrombolytic treatment in a dog model of coronary artery thrombosis can be inhibited with a direct, small molecule thrombin inhibitor (melagatran). Mattsson, C., Björkman, J.A., Abrahamsson, T., Nerme, V., Schatteman, K., Leurs, J., Scharpé, S., Hendriks, D. Thromb. Haemost. (2002) [Pubmed]
  4. Population pharmacokinetics of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, in atrial fibrillation patients receiving long-term anticoagulation therapy. Bååthe, S., Hamrén, B., Karlsson, M.O., Wollbratt, M., Grind, M., Eriksson, U.G. Clinical pharmacokinetics. (2006) [Pubmed]
  5. Inhibition of thrombin abrogates the instant blood-mediated inflammatory reaction triggered by isolated human islets: possible application of the thrombin inhibitor melagatran in clinical islet transplantation. Ozmen, L., Ekdahl, K.N., Elgue, G., Larsson, R., Korsgren, O., Nilsson, B. Diabetes (2002) [Pubmed]
  6. Effects of ximelagatran, an oral direct thrombin inhibitor, r-hirudin and enoxaparin on thrombin generation and platelet activation in healthy male subjects. Sarich, T.C., Wolzt, M., Eriksson, U.G., Mattsson, C., Schmidt, A., Elg, S., Andersson, M., Wollbratt, M., Fager, G., Gustafsson, D. J. Am. Coll. Cardiol. (2003) [Pubmed]
  7. Direct thrombin inhibitor melagatran followed by oral ximelagatran in comparison with enoxaparin for prevention of venous thromboembolism after total hip or knee replacement. Eriksson, B.I., Agnelli, G., Cohen, A.T., Dahl, O.E., Mouret, P., Rosencher, N., Eskilson, C., Nylander, I., Frison, L., Ogren, M. Thromb. Haemost. (2003) [Pubmed]
  8. Different antithrombotic properties of factor Xa inhibitor and thrombin inhibitor in rat thrombosis models. Furugohri, T., Shiozaki, Y., Muramatsu, S., Honda, Y., Matsumoto, C., Isobe, K., Sugiyama, N. Eur. J. Pharmacol. (2005) [Pubmed]
  9. The effects of oral and intravenous direct thrombin inhibitors on the size of photochemically induced cortical infarction in rats. Mikulski, A., Elg, M., Gustafsson, D. Thromb. Res. (2001) [Pubmed]
  10. Effects of melagatran, a novel direct thrombin inhibitor, during experimental septic shock. Eriksson, M., Basu, S., Larsson, A., Mattsson, C., Eriksson, O., Kiiski, R., Nordgren, A. Expert opinion on investigational drugs. (2000) [Pubmed]
  11. No influence of mild-to-moderate hepatic impairment on the pharmacokinetics and pharmacodynamics of ximelagatran, an oral direct thrombin inhibitor. Wåhlander, K., Eriksson-Lepkowska, M., Frison, L., Fager, G., Eriksson, U.G. Clinical pharmacokinetics. (2003) [Pubmed]
  12. Effects of melagatran, a new low-molecular-weight thrombin inhibitor, on thrombin and fibrinolytic enzymes. Gustafsson, D., Antonsson, T., Bylund, R., Eriksson, U., Gyzander, E., Nilsson, I., Elg, M., Mattsson, C., Deinum, J., Pehrsson, S., Karlsson, O., Nilsson, A., Sörensen, H. Thromb. Haemost. (1998) [Pubmed]
  13. Effect of recombinant factor VIIa on melagatran-induced inhibition of thrombin generation and platelet activation in healthy volunteers. Wolzt, M., Levi, M., Sarich, T.C., Boström, S.L., Eriksson, U.G., Eriksson-Lepkowska, M., Svensson, M., Weitz, J.I., Elg, M., Wåhlander, K. Thromb. Haemost. (2004) [Pubmed]
  14. Influence of lepirudin, argatroban, and melagatran on prothrombin time and additional effect of oral anticoagulation. Fenyvesi, T., Joerg, I., Harenberg, J. Clin. Chem. (2002) [Pubmed]
  15. Additive effects of anticoagulants: recombinant human activated protein C and heparin or melagatran, in tissue factor-activated umbilical-cord plasma. Koestenberger, M., Gallistl, S., Muntean, W., Leschnik, B., Fritsch, P., Cvirn, G. Thromb. Haemost. (2005) [Pubmed]
  16. Ximelagatran, an oral direct thrombin inhibitor, has a low potential for cytochrome P450-mediated drug-drug interactions. Bredberg, E., Andersson, T.B., Frison, L., Thuresson, A., Johansson, S., Eriksson-Lepkowska, M., Larsson, M., Eriksson, U.G. Clinical pharmacokinetics. (2003) [Pubmed]
  17. The antithrombotic effect of melagatran in combination with clopidogrel and/or aspirin (carotid artery primary thrombosis study). Hong, T.T., Huang, J., Driscoll, E., Lucchesi, B.R. J. Cardiovasc. Pharmacol. (2005) [Pubmed]
  18. The oral direct thrombin inhibitor, ximelagatran, an alternative for anticoagulant treatment during the puerperium and lactation. Hellgren, M., Johansson, S., Eriksson, U.G., Wåhlander, K. BJOG : an international journal of obstetrics and gynaecology. (2005) [Pubmed]
  19. Small, noncovalent serine protease inhibitors. Sanderson, P.E. Medicinal research reviews. (1999) [Pubmed]
  20. Significantly lower need for blood transfusions associated with post-operatively initiated subcutaneous melagatran/oral ximelagatran compared with enoxaparin. Eriksson, B.I., Agnelli, G., Cohen, A., Dahl, O., Mouret, P., Rosencher, N., Panfilov, S., Andersson, M. Thromb. Haemost. (2004) [Pubmed]
  21. Influence of erythromycin on the pharmacokinetics of ximelagatran may involve inhibition of p-glycoprotein-mediated excretion. Eriksson, U.G., Dorani, H., Karlsson, J., Fritsch, H., Hoffmann, K.J., Olsson, L., Sarich, T.C., Wall, U., Schützer, K.M. Drug Metab. Dispos. (2006) [Pubmed]
  22. A pharmacokinetic study of the combined administration of amiodarone and ximelagatran, an oral direct thrombin inhibitor. Teng, R., Sarich, T.C., Eriksson, U.G., Hamer, J.E., Gillette, S., Schützer, K.M., Carlson, G.F., Kowey, P.R. Journal of clinical pharmacology. (2004) [Pubmed]
  23. Advances in anticoagulation therapy: the role of selective inhibitors of factor Xa and thrombin in thromboprophylaxis after major orthopedic surgery. Andersen, J.C. Semin. Thromb. Hemost. (2004) [Pubmed]
  24. Effect of melagatran on prothrombin time assays depends on the sensitivity of the thromboplastin and the final dilution of the plasma sample. Mattsson, C., Menschiek-Lundin, A., Wåhlander, K., Lindahl, T.L. Thromb. Haemost. (2001) [Pubmed]
  25. Influence of severe renal impairment on the pharmacokinetics and pharmacodynamics of oral ximelagatran and subcutaneous melagatran. Eriksson, U.G., Johansson, S., Attman, P.O., Mulec, H., Frison, L., Fager, G., Samuelsson, O. Clinical pharmacokinetics. (2003) [Pubmed]
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