Eighty years of oral anticoagulation: Learning from history

Maria Rosa Montinari1, Sergio Minelli2, Raffaele De Caterina3

  • 1Chair of History of Medicine, Department of Biological and Environmental Science and Technology, University of Salento, Lecce, Italy.

Vascular Pharmacology
|September 19, 2021
PubMed

Insights

The evolution of oral anticoagulants, from vitamin K antagonists (VKAs) to newer non-vitamin K antagonist oral anticoagulants (NOACs), has transformed thromboembolic disease treatment. Future research focuses on even safer anticoagulants targeting intrinsic pathway factors.

Area of Science:

  • Cardiology
  • Hematology
  • Pharmacology

Background:

  • Vitamin K antagonists (VKAs) have been the primary oral anticoagulants for thromboembolic disease prevention and treatment for 80 years.
  • The development of oral anticoagulants represents a significant advancement in medical history, addressing thrombosis since antiquity.
  • Historically, VKAs were the sole oral anticoagulants available for clinical use.

Purpose of the Study:

  • To review the historical evolution of oral anticoagulant therapy.
  • To highlight the transition from VKAs to non-vitamin K antagonist oral anticoagulants (NOACs).
  • To discuss emerging research in developing novel anticoagulants with improved safety profiles.

Main Methods:

  • This review synthesizes historical data and clinical trial outcomes.
  • It traces the development and adoption of different classes of oral anticoagulants.
  • It examines current research trends in anticoagulant drug discovery.

Main Results:

  • The clinical use of VKAs has declined with the rise of NOACs, supported by large randomized controlled trials.
  • NOACs offer an alternative to VKAs in managing various thromboembolic conditions.
  • Newer anticoagulants targeting factors XI and XII are under investigation for enhanced safety and efficacy.

Conclusions:

  • Oral anticoagulant therapy has undergone significant evolution, improving the management of thromboembolic disorders.
  • The shift from VKAs to NOACs marks a major advancement in patient care.
  • Ongoing research promises the development of next-generation anticoagulants with reduced bleeding risks.

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