Target intelligence / Profile preview

Coagulation factor Xa and Thrombin (Factor Xa and Thrombin)

Target
Factor Xa and Thrombin
Molecular classification
Enzyme, Serine protease, Coagulation factor
01

Overview

Coagulation factor Xa is an activated serine protease that occupies a pivotal position in the coagulation cascade, integrating signals from intrinsic and extrinsic pathways to catalyze the conversion of prothrombin to thrombin. This reaction is greatly amplified in the prothrombinase complex, comprised of factor Xa and its cofactor, factor Va, on platelet membrane surfaces. Thrombin is the final effector of the cascade, executing the conversion of fibrinogen to fibrin, enabling clot formation, and activating platelets and other coagulation factors. Both proteins also participate in cellular signaling, tissue repair, and pathological processes such as inflammation and atherosclerosis. As such, they are key targets for anticoagulant therapies used in cardiovascular disease, stroke prevention, and thromboembolic disorders.

Other names
FXaActivated factor XStuart factorFactor IIaActivated coagulation factor II
02

Mechanism of action

Factor Xa inhibitors: Inhibit the proteolytic activity of FXa, blocking conversion of prothrombin to thrombin, thereby preventing fibrin formation and clot propagation. Thrombin inhibitors: Directly inhibit thrombin's activity, preventing conversion of fibrinogen to fibrin and reducing platelet activation.

03

Biological functions

Activation of prothrombin to thrombinBlood coagulationAmplification of the coagulation cascadePlatelet activation (by generation of thrombin)Tissue remodeling, inflammation, angiogenesisCleavage of fibrinogen to fibrinPlatelet activation (potent agonist)Cellular signaling (via PAR receptors)Inflammation, tissue repair
04

Disease associations

Cardiovascular disease (thrombosis, atherothrombosis, stroke, myocardial infarction)Venous thromboembolism (deep vein thrombosis, pulmonary embolism)Ischemic strokeAcute coronary syndromeAtherosclerosisPotential roles in inflammation and tissue remodeling
05

Safety considerations

Bleeding risk: All FXa and thrombin inhibitors may increase risk of serious bleedingReversal agents: Some have limited options for rapid reversal in the event of bleeding (e.g., andexanet alfa for FXa inhibitors, idarucizumab for dabigatran)Hepatotoxicity: Ximelagatran withdrawn due to liver toxicityDrug interactions: Especially with other anticoagulants or drugs affecting hemostasis
06

Interacting drugs

Rivaroxaban

11 more in the full profile.

07

Biomarkers

Factor Xa activity (for monitoring efficacy)Thrombin generation assaysD-dimer (fibrin degradation product)

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