Development of DX-9065a, a novel direct factor Xa antagonist, in cardiovascular disease.
The development of anticoagulants for treating patients with atherothrombotic disorders of the arterial circulatory system has focused, either directly or indirectly, on thrombin - a pleuripotential effector enzyme with prothrombotic and proinflammatory properties. The pivotal role of factor (f) Xa in thrombin generation, coupled with its direct cellular effects and widely recognized limitations of currently available anticoagulants, has led to the development of pharmacologic inhibitors of this important protease. The following review focuses on DX-9065a - first in a class of direct, selective and reversible fXa antagonists - and its potential applications in the management of patients with cardiovascular disease.
Becker
Richard C
RC
Cardiovascular Thrombosis Center, Duke University Medical Center, Durham, NC 27715, USA. Becke021@mc.duke.edu
Alexander
John
J
Dyke
Christopher K
CK
Harrington
Robert A
RA
D000818:Animals; D000925:Anticoagulants / Q000494:pharmacology*; D019540:Area Under Curve; D001777:Blood Coagulation; D002318:Cardiovascular Diseases / Q000188:drug therapy*; D002986:Clinical Trials as Topic; D003324:Coronary Artery Disease / Q000188:drug therapy; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D015951:Factor Xa / Q000737:chemistry; D065427:Factor Xa Inhibitors; D006801:Humans; D019934:International Normalized Ratio; D051379:Mice; D008954:Models, Biological; D008956:Models, Chemical; D009281:Naphthalenes / Q000494:pharmacology*; D010865:Pilot Projects; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D011422:Propionates / Q000494:pharmacology*; D051381:Rats; D013917:Thrombin / Q000378:metabolism; D013925:Thromboplastin / Q000378:metabolism; D013927:Thrombosis; D013997:Time Factors
C086910:(2S)-2-(4-(((3S)-1-acetimidoyl-3-pyrrolidinyl)oxy)phenyl)-3-(7-amidino-2-naphtyl)propanoic acid; D000925:Anticoagulants; D065427:Factor Xa Inhibitors; D009281:Naphthalenes; D010975:Platelet Aggregation Inhibitors; D011422:Propionates; D013925:Thromboplastin; D013917:Thrombin; D015951:Factor Xa