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VICB Seminar, Jing Yang, Bristol-Myers Squibb: 'The Discovery of Orally Active Small Molecule PAR4 Antagonists'

Wednesday, February 13, 2019,

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  • Location: Biological Sciences Building/Medical Research Building (MRB) III • 465 21st Ave S • Nashville, TN 37232
  • Room: 1220

  The Vanderbilt Institute of Chemical Biology (VICB) presents Dr. Jing Yang, Bristol-Myers Squibb: "The Discovery of Orally Active Small Molecule PAR4 Antagonists"

Key Lecture Points:

The balance between antithrombotic efficacy and bleeding with currently available antiplatelet drugs is suboptimal and many patients remain at high risk of future atherothrombotic events. Thus there is a clear need for newer agents that can provide equivalent or superior antithrombotic efficacy with a lower bleeding profile. Our research is focused on protease-activated receptor 4 (PAR4), a low affinity thrombin receptor, as a promising antiplatelet drug target to provide a potentially safer treatment for
arterial thrombosis. Below is an outline of our research: 

· Discovery of first-in-class orally ctive, potent and selective PAR4 antagonists including BMS-986120
· Preclinical studies of PAR4 antagonist in non-human primate thrombosis and hemostasis models
· Antithrombotic effect of BMS-986120 in human ex vivo thrombosis chamber study
· First-in-human tolerability, PKPD and gene
  variant effects of BMS-986120