Abstract
Ischemic heart disease and cerebrovascular disease are the leading causes of death in the world. Surprisingly, these diseases are treated by relatively antiquated drugs. However, due to our improved understanding of the underlying pathology of these diseases, and a number of technological advances in tools for drug discovery and chemical optimization, an exciting new wave of antithrombotic compounds is beginning to emerge in clinical trials. These agents, referred to as direct coagulation factor Xa inhibitors, appear to provide an enhanced risk-benefit margin compared to conventional therapy. Preclinical and early clinical data gathered over the past few years suggests that direct fXa inhibitors will provide the necessary advancements in efficacy, safety, and ease of use required to displace conventional therapy. Whether or not these agents will succeed will be determined as this class of agents advances through clinical trials in the near future. This review describes some of the key studies that sparked an interest in fXa as a therapeutic target, highlighting the findings that provided important rationale for continuing the development of potent and selective direct fXa inhibitors.
Keywords: ANTITHROMBOTIC EFFICACY, Anticoagulants
Current Topics in Medicinal Chemistry
Title: Coagulation Factor Xa Inhibition: Biological Background and Rationale
Volume: 1 Issue: 2
Author(s): Robert J. Leadley, Jr.
Affiliation:
Keywords: ANTITHROMBOTIC EFFICACY, Anticoagulants
Abstract: Ischemic heart disease and cerebrovascular disease are the leading causes of death in the world. Surprisingly, these diseases are treated by relatively antiquated drugs. However, due to our improved understanding of the underlying pathology of these diseases, and a number of technological advances in tools for drug discovery and chemical optimization, an exciting new wave of antithrombotic compounds is beginning to emerge in clinical trials. These agents, referred to as direct coagulation factor Xa inhibitors, appear to provide an enhanced risk-benefit margin compared to conventional therapy. Preclinical and early clinical data gathered over the past few years suggests that direct fXa inhibitors will provide the necessary advancements in efficacy, safety, and ease of use required to displace conventional therapy. Whether or not these agents will succeed will be determined as this class of agents advances through clinical trials in the near future. This review describes some of the key studies that sparked an interest in fXa as a therapeutic target, highlighting the findings that provided important rationale for continuing the development of potent and selective direct fXa inhibitors.
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Cite this article as:
Leadley, Jr. Robert J., Coagulation Factor Xa Inhibition: Biological Background and Rationale, Current Topics in Medicinal Chemistry 2001; 1 (2) . https://dx.doi.org/10.2174/1568026013395380
DOI https://dx.doi.org/10.2174/1568026013395380 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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