Target intelligence / Profile preview

Coagulation factor Xa–Antithrombin III complex (FXa-ATIII)

Target
FXa-ATIII
Molecular classification
Enzyme-inhibitor complex, Serine protease-serpin complex, Protein complex
01

Overview

The Coagulation factor Xa–Antithrombin III complex is a critical regulatory assembly in the human blood coagulation cascade. It consists of the activated serine protease Factor Xa (FXa) and its primary endogenous inhibitor, Antithrombin III (ATIII), a member of the serpin superfamily. Factor Xa is responsible for the conversion of prothrombin to thrombin, a pivotal step in clot formation. Antithrombin III neutralizes Factor Xa by forming an initial, reversible encounter complex that transitions into a stable, inactive covalent complex, thereby preventing excessive thrombus propagation (Source: UniProt P01008, P00742). This interaction is the pharmacological basis for indirect anticoagulants like heparin and fondaparinux. These drugs bind to ATIII, inducing a conformational change that increases its affinity for Factor Xa by several thousand-fold, effectively accelerating the formation of the encounter complex (Source: PubMed PMID: 15670155). Monitoring the levels of this complex serves as a clinical biomarker for intravascular coagulation activation and the efficacy of antithrombotic therapies (Source: StatPearls, Heparin).

Other names
Factor Xa-Antithrombin complexFXa-AT complexAntithrombin-Factor Xa complexFactor Xa-Antithrombin III encounter complex
02

Mechanism of action

Indirect inhibition of Factor Xa through allosteric potentiation of Antithrombin III, accelerating the formation of the encounter complex and subsequent covalent inactivation.

03

Biological functions

Regulation of blood coagulationProteolysis inhibitionHemostasisNegative regulation of coagulation cascade
04

Disease associations

Venous thromboembolismPulmonary embolismAtrial fibrillationMyocardial infarctionDisseminated intravascular coagulationAntithrombin III deficiency
05

Safety considerations

HemorrhageHeparin-induced thrombocytopenia (HIT)Osteoporosis (with long-term use)Hypersensitivity reactions
06

Interacting drugs

Heparin

5 more in the full profile.

07

Biomarkers

FXa-ATIII complex levelsAnti-Xa activityProthrombin fragment 1+2D-dimer

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