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

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Abstract

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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Authors and Affiliations

  1. Research and Development (retired), Bristol Myers Squibb Company, P.O. Box 5400, Princeton, NJ, 08543, USA

    Robert M. Knabb

  2. Small Molecule Drug Discovery, Research and Early Development, Bristol Myers Squibb Company, P.O. Box 5400, Princeton, NJ, 08543, USA

    Ruth R. Wexler

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  1. Robert M. Knabb
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  2. Ruth R. Wexler
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Correspondence to Ruth R. Wexler.

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Knabb, R.M., Wexler, R.R. From basic science to life-saving therapy: the rationale, and drug discovery efforts that led to the direct factor Xa inhibitor eliquis. J Thromb Thrombolysis 52, 403–407 (2021). https://doi.org/10.1007/s11239-021-02529-w

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  • DOI: https://doi.org/10.1007/s11239-021-02529-w

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