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Review
. 2022 Oct 13;11(20):3214.
doi: 10.3390/cells11203214.

Anticoagulants: A Short History, Their Mechanism of Action, Pharmacology, and Indications

Marco Heestermans  1   2 , Géraldine Poenou  2   3 , Hind Hamzeh-Cognasse  2 , Fabrice Cognasse  1   2 , Laurent Bertoletti  2   3   4
Affiliations
Review

Anticoagulants: A Short History, Their Mechanism of Action, Pharmacology, and Indications

Marco Heestermans et al. Cells. .

Abstract

Anticoagulant drugs antagonize coagulation and are used to prevent or cure (recurrent) venous thromboembolism (VTE). Drugs to prevent clotting have been used for more than a century, and, nowadays, physicians possess a broad panel of multiple anticoagulants to meet the individual needs of a patient. Within this review, we aimed to revise the history of the different anticoagulants that are currently prescribed in the clinic. In addition, we compared their pharmacological properties, medical indications, and the difficulties in implementing new anticoagulants in vulnerable patient populations. Since the introduction of unfractionated heparin in the 1930s, major advances in the mechanistic understanding and the medical use of anticoagulants have allowed for significant improvements to treat VTE patients. However, a new generation of anticoagulants is currently being tested in clinical trials, with the goal of further optimizing medical care.

Keywords: DOACs; anticoagulant drugs; drug–drug interactions; heparin; novel anticoagulants; pharmacology; venous thromboembolism; vitamin K antagonists.

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Conflict of interest statement

The authors declare no conflicts of interest.

Figures

Figure 1
Figure 1
Anticoagulants and their targets within the coagulation cascade. The coagulation cascade consists of three parts: the tissue factor (TF) pathway, the contact activation pathway, and the common pathway. Currently used anticoagulants target primarily coagulation factors from the common pathway: FXa (apixaban, edoxaban, fondaparinux, and rivaroxaban) and thrombin (FIIa; dabigatran, bilvalirudin, and argatroban). UFH, VKA, and LMWH have multiple targets within the coagulation cascade. Anticoagulants that are currently under development or undergoing clinical trials target factors from the TF pathway (TF-FVIIa complex) or the contact activation pathway (FIXa, FXIa, and FXIIa). Tenase complex: FVIIIa-FIXa complex. Prothrombinase complex: FVIIIa-FIXa-FXa complex.
See this image and copyright information in PMC

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