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lüll Factor IXa inhibitors as novel anticoagulants Howard EL; Becker KC; Rusconi CP; Becker RCArterioscler Thromb Vasc Biol 2007[Apr]; 27 (4): 722-7Currently available anticoagulants are limited by modest therapeutic benefits, narrow clinical applications, increased bleeding risk, and drug-induced thrombophilia. Because factor IX plays a pivotal role in tissue factor (TF)-mediated thrombin generation, it may represent a promising target for drug development. Several methods of attenuating factor IX activity, including monoclonal antibodies, synthetic active site-blocked competitive inhibitors, oral inhibitors, and RNA aptamers, have undergone investigation. This review summarizes present knowledge of factor IX inhibitors with emphasis on biology, pharmacology, preclinical data, and early-phase clinical experience in humans.|Animals[MESH]|Antibodies, Monoclonal/pharmacology[MESH]|Anticoagulants/*pharmacology[MESH]|Aptamers, Nucleotide/pharmacology[MESH]|Blood Coagulation/physiology[MESH]|Factor IX/chemistry/physiology[MESH]|Factor IXa/*antagonists & inhibitors/immunology[MESH]|Humans[MESH]|Structure-Activity Relationship[MESH] |