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Updated: Aug 8, 2026
13:08
Measurement of Factor V Activity in Human Plasma Using a Microplate Coagulation Assay
Published on: September 9, 2012
Factor Xa inhibitors (Berlex)
1Lilly Research Centre, Erl Wood Manor, Sunninghill Road, Windelsham, Surrey, GU20 6PH, UK. Lewis_Richard@Lilly.com
Idrugs : the Investigational Drugs Journal
|August 16, 2005
Summary
Berlex Biosciences is developing novel Factor Xa inhibitors for treating thrombotic disorders. Research focuses on compounds like ZK-805412, showing potent inhibition, and exploring diverse chemical structures for enhanced efficacy.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Biochemistry
Background:
- Thrombotic disorders represent a significant unmet medical need.
- Factor Xa is a key enzyme in the coagulation cascade, making it a therapeutic target.
- Previous research has identified various chemical scaffolds with potential Factor Xa inhibitory activity.
Purpose of the Study:
- To investigate novel series of Factor Xa inhibitors for the prevention and treatment of thrombotic disorders.
- To identify specific compounds with high inhibitory potency against Factor Xa.
Main Methods:
- Structure-based drug design utilizing ZK-805412 as a lead compound.
- Synthesis and evaluation of diverse chemical series, including condensed diphenoxypyridines, indoles, benzimidazoles, and carbazoles.
- In vitro assessment of inhibitory activity against Factor Xa.
Main Results:
- ZK-805412, a Z,Z-2,7-bis(dibenzylidene)cycloheptanone derivative, demonstrated nanomolar potency as a Factor Xa inhibitor.
- Specific inhibitors such as ZK-806350 and ZK-807191 were identified within the program.
- The inhibitory activity of 2,6-diphenoxypyridines on Factor Xa was confirmed in vitro.
Conclusions:
- Berlex Biosciences is actively pursuing the development of potent Factor Xa inhibitors.
- The identified compounds and explored chemical series hold promise for the therapeutic management of thrombotic conditions.
- Collaboration with Warner-Lambert further supports the advancement of these Factor Xa inhibitors.
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