Direct thrombin inhibitors: Patents 2002-2012 (Review)

  • Authors:
    • Yi Kong
    • Hao Chen
    • Yong-Qing Wang
    • Ling Meng
    • Ji-Fu Wei
  • View Affiliations

  • Published online on: March 6, 2014     https://doi.org/10.3892/mmr.2014.2025
  • Pages: 1506-1514
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Abstract

Acute vascular diseases and other thromboses of the blood system constitute major health risks in developing countries. Thrombin plays a central role in blood coagulation, which is a crucial process involved in thrombosis. Direct thrombin inhibitors (DTIs) such as argatroban, dabigatran, dabigatran etexilate, lepirudin, desirudin and bivalirudin, which bind to thrombin and block its enzymatic activity, are widely and effectively used in the treatment of thromboembolic diseases. DTIs appear to overcome the disadvantages of indirect thrombin inhibitors such as unfractionated heparins (UFH). Although these DTIs show specific advantages over indirect inhibitors, they still present limitations, such as a narrow therapeutic window, and bleeding and anaphylaxis as side-effects. Novel anticoagulant drugs need thus to be developed to overcome these limitations. In the search for additional candidate agents with improved efficacy, safety and high bioavailability in oral administration, a high number of compounds has been identified, such as those derived from the tripeptide template D-Phe-Pro-Arg, aptamers and peptides isolated from blood-sucking animals. These candidates may prove the new agents of choice for the treatment of cardiovascular diseases.
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May-2014
Volume 9 Issue 5

Print ISSN: 1791-2997
Online ISSN:1791-3004

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Spandidos Publications style
Kong Y, Chen H, Wang Y, Meng L and Wei J: Direct thrombin inhibitors: Patents 2002-2012 (Review). Mol Med Rep 9: 1506-1514, 2014.
APA
Kong, Y., Chen, H., Wang, Y., Meng, L., & Wei, J. (2014). Direct thrombin inhibitors: Patents 2002-2012 (Review). Molecular Medicine Reports, 9, 1506-1514. https://doi.org/10.3892/mmr.2014.2025
MLA
Kong, Y., Chen, H., Wang, Y., Meng, L., Wei, J."Direct thrombin inhibitors: Patents 2002-2012 (Review)". Molecular Medicine Reports 9.5 (2014): 1506-1514.
Chicago
Kong, Y., Chen, H., Wang, Y., Meng, L., Wei, J."Direct thrombin inhibitors: Patents 2002-2012 (Review)". Molecular Medicine Reports 9, no. 5 (2014): 1506-1514. https://doi.org/10.3892/mmr.2014.2025