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Chemical Compound Review

Dabigatran     3-[[2-[[(4- carbamimidoylphenyl) amino]methy...

Synonyms: BIBR-953, SureCN3573, BIBR953, CHEMBL48361, S2196_Selleck, ...
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Disease relevance of Dabigatran


High impact information on Dabigatran

  • Aims To describe the pharmacokinetic-pharmacodynamic (PK-PD) characteristics of the direct thrombin inhibitor dabigatran in hip replacement patients by assessing coagulation parameters activated partial thromboplastin time (aPTT) and ecarin clotting time (ECT), interindividual variability and factors affecting PD responses [2].
  • The AUC(0-24) of dabigatran was 88% of the steady-state AUC using a preliminary tablet formulation and 106% of that seen in the healthy volunteer study [3].
  • In an open-label, 3-way crossover study, dabigatran etexilate was administered to 18 male volunteers in the fasted state, after administration of food and with coadministration of the proton pump inhibitor, pantoprazole [3].

Gene context of Dabigatran

  • When treated with dabigatran (1 microg/ml), scleroderma lung myofibroblasts produced 6-fold less alpha-SMA, 3-fold less CTGF, and 2-fold less type I collagen compared with untreated cells [4].

Analytical, diagnostic and therapeutic context of Dabigatran


  1. A new oral direct thrombin inhibitor, dabigatran etexilate, compared with enoxaparin for prevention of thromboembolic events following total hip or knee replacement: the BISTRO II randomized trial. Eriksson, B.I., Dahl, O.E., Büller, H.R., Hettiarachchi, R., Rosencher, N., Bravo, M.L., Ahnfelt, L., Piovella, F., Stangier, J., Kälebo, P., Reilly, P. J. Thromb. Haemost. (2005) [Pubmed]
  2. Effects of the direct thrombin inhibitor dabigatran on ex vivo coagulation time in orthopaedic surgery patients: a population model analysis. Liesenfeld, K.H., Sch??fer, H.G., Troc??niz, I.F., Tillmann, C., Eriksson, B.I., Stangier, J. British journal of clinical pharmacology. (2006) [Pubmed]
  3. Pharmacokinetic profile of the oral direct thrombin inhibitor dabigatran etexilate in healthy volunteers and patients undergoing total hip replacement. Stangier, J., Eriksson, B.I., Dahl, O.E., Ahnfelt, L., Nehmiz, G., Stähle, H., Rathgen, K., Svärd, R. Journal of clinical pharmacology. (2005) [Pubmed]
  4. Dabigatran, a direct thrombin inhibitor, demonstrates antifibrotic effects on lung fibroblasts. Bogatkevich, G.S., Ludwicka-Bradley, A., Silver, R.M. Arthritis Rheum. (2009) [Pubmed]
  5. Prevention of venous thromboembolism following orthopaedic surgery: clinical potential of direct thrombin inhibitors. Eriksson, B.I., Dahl, O.E. Drugs (2004) [Pubmed]
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