Darexaban
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Preferred IUPAC name
N-[2-Hydroxy-6-(4-methoxybenzamido)phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide | |
Other names
YM150
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Identifiers | |
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3D model (
JSmol ) |
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ChemSpider | |
PubChem CID
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UNII |
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Properties | |
C27H30N4O4 | |
Molar mass | 474.561 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Darexaban (YM150) is a direct inhibitor of
Clinical uses
Atrial fibrillation
Atrial fibrillation is an abnormal heart rhythm that causes a reduction in the cardiac output and blood flow to the brain. It also promotes the formation of blood clots in the atrial chambers of the heart.[4] Atrial fibrillation is associated with an increased risk of embolic stroke due to the increased risk of blood clot development.[5] Oral anticoagulant drugs such as Darexaban decrease the incidence and severity of stroke in patients with atrial fibrillation by preventing the formation of blood clots.[6]
Contraindictions
The RUBY-1 phase II trial results show that oral administration of darexaban in combination with the standard
Pharmacology
Mechanism of action
Factor Xa (FXa) is an essential blood coagulation factor
Darexaban and darexaban glucuronide selectively and competitively inhibit FXa, suppressing prothrombin activity at the sites of blood clot (thrombus) formation. This leads to a decrease in blood clot formation in a dose dependent manner.[2] Reducing blood clot formation will decrease blood flow blockages, thus possibly lowering the risk of myocardial infarction, unstable angina, venous thrombosis, and ischemic stroke.[8]
Pharmacokinetics
Darexaban is rapidly absorbed and extensively metabolized in the liver to its active metabolite, darexaban
References
- S2CID 2343858.
- ^ PMID 22040919.
- ^ S2CID 1643706.
- ^ ISBN 978-0071604055.
- PMID 9518970.
- PMID 12968085.
- ^ PMID 21878434.)
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: CS1 maint: numeric names: authors list (link - PMID 21995444.
- S2CID 21184977.)
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: CS1 maint: numeric names: authors list (link