From basic science to life-saving therapy: the rationale, and drug discovery efforts that led to the direct factor Xa inhibitor eliquis

Over the past few decades, drug discovery directed at the treatment and prevention of thromboembolic diseases has been challenged by the need to balance robust efficacy with improved safety relative to the standard of care. To this end, the most impactful advance to date has been the discovery and d...

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Published inJournal of thrombosis and thrombolysis Vol. 52; no. 2; pp. 403 - 407
Main Authors Knabb, Robert M., Wexler, Ruth R.
Format Journal Article
LanguageEnglish
Published New York Springer US 01.08.2021
Springer Nature B.V
Subjects
Anticoagulants
Cardiology
Disease prevention
Drug Discovery
Enzymes
Factor Xa Inhibitors - therapeutic use
Hematology
Humans
Medicine
Medicine & Public Health
Peptides
Pyrazoles
Pyridones
R&D
Research & development
Stroke
Thromboembolism
Thrombosis
Protease
Thrombosis
Eliquis
Factor Xa inhibitor
Apixaban
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Summary:Over the past few decades, drug discovery directed at the treatment and prevention of thromboembolic diseases has been challenged by the need to balance robust efficacy with improved safety relative to the standard of care. To this end, the most impactful advance to date has been the discovery and development of oral factor Xa inhibitors. In this essay, a brief account of the program that culminated in the discovery of Eliquis (apixaban) and the commitment to identify a compound with an optimal profile are described.
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ISSN:0929-5305
1573-742X
DOI:10.1007/s11239-021-02529-w