Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.

Wu Yang,Yufeng Wang,Amy Lai,Charles G. Clark,James R. Corte,Tianan Fang,Paul J. Gilligan,Yoon T. Jeon,Kumar Balashanmuga Pabbisetty,Richard Rampulla,Arvind Mathur,Mahammed Kaspady,Premsai Rai Neithnadka,Arunachalam Arumugam,Sivashankaran Raju,Karen A. Rossi,Joseph E. Myers,Steven Sheriff,Zhen Lou,Joanna J. Zheng,Silvi A. Chacko,Jeffrey M. Bozarth,Yiming Wu,Earl J. Crain,Pancras C. Wong,Dietmar A. Seiffert,Joseph M. Luettgen,Patrick Y. S. Lam,Ruth R. Wexler,William R. Eiwng

Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.

2020

Oral factor XIa (FXIa) inhibitors may provide a promising new antithrombotic therapy with an improved benefit to bleeding risk profile over existing antithrombotic agents. Herein, we report applica...

Keywords:

Factor XIa
Biochemistry
Bioavailability
Chemistry
Antithrombotic
risk profile

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