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Brief Reviews |
From the Department of Pathology, Duke University Medical Center, Durham, NC; Department of Chemistry, Boston University, Mass; Regado Biosciences Inc, Durham, NC; and Department of Medicine, Divisions of Cardiology and Hematology, Duke University Medical Center, Durham, NC.
Correspondence to Richard C. Becker, MD, Professor of Medicine, Duke University School of Medicine, Director, Cardiovascular Thrombosis Center, Duke University Medical School, 2400 Pratt St, Durham, NC 27710. E-mail becke021{at}mc.duke.edu
Series Editor: Jeffrey I. Weitz
Emerging Anticoagulant Drugs
ATVB In Focus
Currently 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.
This review summarizes factor IXa inhibitors, an emerging class of anticoagulants that includes active site-blocked inhibitors, monoclonal antibodies, oral inhibitors, and RNA aptamers.
Key Words: anticoagulants coagulation factor IX (fIX), monoclonal antibodies (mAb), RNA aptamers
Related Article:
Arterioscler. Thromb. Vasc. Biol. 2007 27: 721.
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