New developments in anticoagulants: Past, present and future

Thromb Haemost. 2017 Jun 28;117(7):1283-1288. doi: 10.1160/TH16-10-0807. Epub 2017 Jun 8.

Abstract

Thrombosis is a leading cause of death and disability worldwide, and anticoagulants are the mainstay of its prevention and treatment. Starting with unfractionated heparin (UFH) and vitamin K antagonists (VKAs) such as warfarin, the choices of anticoagulants have exploded in the past 20 years. With over 90 % subcutaneous bioavailability, no need for coagulation monitoring and dose adjustment, and a lower risk of heparin-induced thrombocytopenia, low-molecular-weight heparin and fondaparinux have replaced UFH for prevention and initial treatment of venous thromboembolism and for secondary prevention in cancer patients. In patients undergoing percutaneous interventions, bivalirudin is often used instead of UFH. Oral anticoagulation therapy has advanced with the introduction of the non-vitamin K antagonist oral anticoagulants (NOACs), which include dabigatran, rivaroxaban, apixaban and edoxaban. With efficacy at least equal to that of VKAs but with greater safety and convenience, the NOACs are now replacing VKAs for many indications. This paper a) highlights these advances, b) outlines how specific reversal agents for the NOACs will enhance their safety, c) reviews some of the ongoing trials with the NOACs, and d) describes the inhibitors of factor XII and XI that are under investigation as anticoagulants.

Keywords: Thrombosis; anticoagulant; heparin; low-molecular-weight heparin; non-vitamin K antagonist oral anticoagulant; warfarin.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anticoagulants / administration & dosage
  • Anticoagulants / adverse effects
  • Anticoagulants / therapeutic use*
  • Antidotes / therapeutic use
  • Coronary Artery Disease / drug therapy
  • Drug Discovery
  • Factor XI / antagonists & inhibitors
  • Factor XII / antagonists & inhibitors
  • Heart Failure / drug therapy
  • Heparin / adverse effects
  • Humans
  • Peripheral Arterial Disease / drug therapy
  • Stroke / drug therapy
  • Thrombosis / blood
  • Thrombosis / drug therapy
  • Thrombosis / prevention & control
  • Venous Thromboembolism / drug therapy
  • Vitamin K / antagonists & inhibitors
  • Warfarin / adverse effects

Substances

  • Anticoagulants
  • Antidotes
  • Vitamin K
  • Warfarin
  • Factor XII
  • Heparin
  • Factor XI