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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.