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      Factor XI(a) inhibitors for thrombosis: an updated patent review (2016-present)

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      Expert Opinion on Therapeutic Patents

      Informa UK Limited

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          Abstract

          Anticoagulation without bleeding is an ideal goal in treating thrombosis, however, this goal has not been achieved. All current anticoagulants are associated with significant bleeding which limits their safe use. Genetic and pharmacological findings indicate that factor XIa is a key player in thrombosis, yet it is a relatively marginal one in hemostasis. Thus, factor XIa and its zymogen offer a unique opportunity to develop anticoagulants with low bleeding risk. A survey of patent literature has retrieved more than 50 patents on the discovery of novel therapeutics targeting factor XI(a) since 2016. Small molecules, monoclonal antibodies, oligonucleotides, and polypeptides have been developed to inhibit factor XI(a). Many inhibitors are in early development and few have been evaluated in clinical trials. Factor XI(a) is being actively pursued as a drug target for the development of effective and safer anticoagulants. Although many patents claiming factor XI(a) inhibitors were filed prior to 2016, recent literature reveals a moderately declining trend. Nevertheless, more agents have entered different levels of clinical trials. These agents exploit diverse mechanistic strategies for inhibition. Although further development is warranted, reaching one or more of these agents to the clinic will transform the anticoagulation therapy.

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          Contributors
          (View ORCID Profile)
          Journal
          Expert Opinion on Therapeutic Patents
          Expert Opinion on Therapeutic Patents
          Informa UK Limited
          1354-3776
          1744-7674
          January 02 2020
          December 19 2019
          January 02 2020
          : 30
          : 1
          : 39-55
          Affiliations
          [1 ]Division of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, New Orleans, LA, USA
          Article
          10.1080/13543776.2020.1705783
          7515655
          31847619
          © 2020

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