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New antithrombin‐based anticoagulants
Author(s) -
Desai Umesh R.
Publication year - 2004
Publication title -
medicinal research reviews
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.868
H-Index - 130
eISSN - 1098-1128
pISSN - 0198-6325
DOI - 10.1002/med.10058
Subject(s) - antithrombin , antithrombotic , heparin , coagulation , anticoagulant , thrombin , pharmacology , chemistry , discovery and development of direct thrombin inhibitors , biochemistry , medicine , immunology , platelet , surgery
Clinically used anticoagulants are inhibitors of enzymes involved in the coagulation pathway, primarily thrombin and factor Xa. These agents can be either direct or indirect inhibitors of clotting enzymes. Heparin‐based anticoagulants are indirect inhibitors that enhance the proteinase inhibitory activity of a natural anticoagulant, antithrombin. Despite its phenomenal success, current anticoagulation therapy suffers from the risk of serious bleeding. The need for safer and more effective antithrombotic agents clearly exists. The past decade has seen enormous effort directed toward discovering and/or designing new molecules with anticoagulant activity. These new molecules can be classified into (a) antithrombin and its mutants, (b) natural polysaccharides, (c) synthetic modified heparins and heparin‐mimics, (d) synthetic oligosaccharides, and (e) synthetic non‐sugar antithrombin activators. This review focuses on these efforts in designing or discovering new molecules that act through the antithrombin pathway of anticoagulation. © 2003 Wiley Periodicals, Inc. Med Res Rev, 24, No. 2, 151–181, 2004