Title:Developments of Anticoagulants and New Agents with Anti-Coagulant Effects in Deep Vein Thrombosis
Volume: 17
Issue: 4
Author(s): Yi-Ping Dang, Yun-Fei Chen, Yi-Qing Li and Lei Zhao
Affiliation:
Keywords:
Anticoagulant, anticoagulation potential, deep vein thrombosis, new agent.
Abstract: Deep Vein Thrombosis (DVT) has been known as a common medical problem all over the
world. Thrombus traveling in blood vessels may lead to pulmonary embolism (PE), associated with high
rates of mortality. Anticoagulant therapy is the mainstay treatment of DVT. Common anticoagulants,
Vitamin K antagonists (VKAs), unfractionated heparin (UFH) and Low-molecular-weight heparin
(LMWH) have been used in clinical application over decades, but can increase the risk of hemorrhage.
Thereby, several new oral anticoagulants (NOACs) have been developed, which includes direct
thrombin inhibitors (DTI) and direct factor Xa inhibitors. To be contrast with VKAs and UFH, NOACs
have many advantages such as rapid offset action, few drug/food interactions and no need for routine
coagulation monitoring, etc. Many NOACs are still being evaluated in Phase III clinical trials such as
Betrixaban and Darexaban (YM150). However, NOACs still have problems to be solved such as lack of
antidotes and laboratory monitoring, high drug costs, etc. Besides, several agents have already shown
the potential to be new anticoagulants. Factor Xa play an important role in thrombin generation and
coagulation pathway. Thus, the new compounds directly targeting on factor Xa for prevention DVT are
highly anticipated. DPC423, a new series of 6-substituted coumarin derivatives and Phenyltriazolinones
as potent factor Xa inhibitors have been recently reported. Recent studies revealed that agents extracted
from botanicals not only have anti-coagulant effects but also possess other pharmacological activities
such as anti-inflammation to alleviate the post-thrombotic syndromes. All the evidence above suggests
that many new compounds might have great potential to be more effective and safe oral anticoagulants.