Factor XIa Inhibitors as New Anticoagulants

J Med Chem. 2018 Sep 13;61(17):7425-7447. doi: 10.1021/acs.jmedchem.8b00173. Epub 2018 May 18.

Abstract

With the introduction of thrombin and factor Xa inhibitors to the oral anticoagulant market, significant improvements in both efficacy and safety have been achieved. Early clinical and preclinical data suggest that inhibitors of factor XIa can provide a still safer alternative, with expanded efficacy for arterial indications. This Perspective provides an overview of target rationale and details of the discovery and development of inhibitors of factor XIa as next generation antithrombotic agents.

Publication types

  • Review

MeSH terms

  • Antibodies, Monoclonal / chemistry
  • Antibodies, Monoclonal / pharmacology
  • Anticoagulants / chemistry*
  • Anticoagulants / pharmacology*
  • Aptamers, Nucleotide / chemistry
  • Aptamers, Nucleotide / pharmacology
  • Catalytic Domain
  • Clinical Trials as Topic
  • Factor XIa / antagonists & inhibitors*
  • Factor XIa / chemistry
  • Factor XIa / metabolism
  • Humans
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology

Substances

  • Antibodies, Monoclonal
  • Anticoagulants
  • Aptamers, Nucleotide
  • Small Molecule Libraries
  • Factor XIa