PMID- 16146728
OWN - NLM
STAT- MEDLINE
DCOM- 20060602
LR  - 20190902
IS  - 1093-9946 (Print)
IS  - 1093-4715 (Linking)
VI  - 11
DP  - 2006 Jan 1
TI  - Factor Xa inhibitors: new anti-thrombotic agents and their characteristics.
PG  - 232-48
AB  - Factor Xa (FXa) is a key enzyme that is positioned at the convergence of the 
      intrinsic and extrinsic pathways in the blood coagulation cascade, and 
      inactivation by a specific FXa inhibitor effectively prevents the generation of 
      thrombin. Various types of low molecular weight (LMW) heparin, which function as 
      semi-selective and indirect FXa inhibitors, are replacing unfractionated heparin 
      (UFH) as agents for the prevention and treatment of venous thromboembolism (VTE), 
      as well as in initial treatment for coronary events. Of those, heparinoid has 
      been shown to be safer and more effective for the prevention of postoperative VTE 
      than UFH, especially for treatment of heparin-induced thrombocytopenia (HIT). 
      Further, synthetic pentasaccharide has been found to offer advantages over 
      current thromboprophylactic regimens in a number of patients undergoing major 
      orthopedic surgery. Other studies have shown that pentasaccharide is more 
      effective for overall VTE in comparison with LMW heparin, though it was also 
      associated with an increased rate of major bleeding. Synthetic, selective, and 
      direct inhibitors to FXa, such as DX-9065a, are highly potent and orally 
      bioavailable antithrombotic agents that have demonstrated an improved side effect 
      profile, probably by allowing sufficient thrombin to remain for platelet 
      activation and normal hemostasis, while preventing pathological thrombus 
      formation. For thrombosis therapy, the most desirable type of antithrombotic 
      agent is an orally active drug that has a broad range of effective doses and no 
      hemorrhagic side effects. Presently, many types of direct inhibitors are in 
      various stages of clinical trials and expected to provide significant benefits as 
      compared to currently utilized therapy strategies.
FAU - Ieko, Masahiro
AU  - Ieko M
AD  - Deaptment of Internal Medicine, School of Dentistry, Health Sciences University 
      of Hokkaido, Ishikari-Tobetsu, Hokkaido, Japan. iekom@hoku-iryo-u.ac.jp
FAU - Tarumi, Takashi
AU  - Tarumi T
FAU - Nakabayashi, Toru
AU  - Nakabayashi T
FAU - Yoshida, Mika
AU  - Yoshida M
FAU - Naito, Sumiyoshi
AU  - Naito S
FAU - Koike, Takao
AU  - Koike T
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20060101
PL  - United States
TA  - Front Biosci
JT  - Frontiers in bioscience : a journal and virtual library
JID - 9709506
RN  - 0 (Anticoagulants)
RN  - 0 (Factor Xa Inhibitors)
RN  - 0 (Fibrinolytic Agents)
RN  - 0 (Heparin, Low-Molecular-Weight)
RN  - 0 (Platelet Aggregation Inhibitors)
RN  - 0 (Polysaccharides)
RN  - 24967-94-0 (Dermatan Sulfate)
RN  - 9005-49-6 (Heparin)
RN  - 9007-28-7 (Chondroitin Sulfates)
RN  - 9050-30-0 (Heparitin Sulfate)
RN  - BI6GY4U9CW (danaparoid)
RN  - J177FOW5JL (Fondaparinux)
SB  - IM
MH  - Animals
MH  - Anticoagulants/therapeutic use
MH  - Bleeding Time
MH  - Blood Coagulation
MH  - Chondroitin Sulfates/therapeutic use
MH  - Clinical Trials as Topic
MH  - Dermatan Sulfate/therapeutic use
MH  - *Factor Xa Inhibitors
MH  - Fibrinolytic Agents/*pharmacology
MH  - Fondaparinux
MH  - Hemostasis
MH  - Heparin/chemistry/therapeutic use
MH  - Heparin, Low-Molecular-Weight/therapeutic use
MH  - Heparitin Sulfate/therapeutic use
MH  - Humans
MH  - Models, Biological
MH  - Models, Chemical
MH  - Platelet Aggregation
MH  - Platelet Aggregation Inhibitors/therapeutic use
MH  - Polysaccharides/chemistry/therapeutic use
MH  - Thromboembolism/drug therapy
RF  - 108
EDAT- 2005/09/09 09:00
MHDA- 2006/06/03 09:00
CRDT- 2005/09/09 09:00
PHST- 2005/09/09 09:00 [pubmed]
PHST- 2006/06/03 09:00 [medline]
PHST- 2005/09/09 09:00 [entrez]
AID - 1794 [pii]
AID - 10.2741/1794 [doi]
PST - epublish
SO  - Front Biosci. 2006 Jan 1;11:232-48. doi: 10.2741/1794.