on February 1, 2007
Published online before print February 1, 2007, doi: 10.1161/01.ATV.0000259363.91070.f1
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Submitted on October 4, 2006
Accepted on January 19, 2007
Factor IXa Inhibitors as Novel Anticoagulants. R1 Howard Factor IXa Inhibitors
Emily L. Howard ;
From the Department of Pathology, Duke University Medical Center, Durham, NC; Department of Chemistry, Boston University, Massachusetts; Regado Biosciences Inc, Durham, NC; and Department of Medicine, Divisions of Cardiology and Hematology, Duke University Medical Center, Durham, NC.
* To whom correspondence should be addressed. E-mail: becke021{at}mc.duke.edu.
Abstract--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 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.
Key words: anticoagulants • coagulation • factor IX (fIX), monoclonal antibodies (mAb), RNA aptamers
Related Article:
- Emerging Anticoagulant Drugs
- Jeffrey I. Weitz
Arterioscler Thromb Vasc Biol 2007 27: 721.[Extract] [Full Text] [PDF]
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