Target intelligence / Profile preview

Coagulation factor IIa and Coagulation factor Xa (FIIa and FXa)

Target
FIIa and FXa
Molecular classification
Enzyme, Serine protease
01

Overview

Coagulation factors IIa (thrombin) and Xa are pivotal serine proteases within the common pathway of the blood coagulation cascade. Factor Xa, once activated from its zymogen form, assembles into the prothrombinase complex to catalyze the conversion of prothrombin (Factor II) into thrombin (Factor IIa). Thrombin serves as the ultimate effector of the cascade, converting soluble fibrinogen into insoluble fibrin to form a stable blood clot, while also activating platelets and providing feedback amplification by activating upstream factors. Due to their central roles in thrombus formation, both factors are major therapeutic targets for anticoagulant drugs. Direct oral anticoagulants (DOACs) like rivaroxaban and apixaban target Factor Xa, while dabigatran targets thrombin, providing effective prevention and treatment for conditions such as venous thromboembolism and stroke in atrial fibrillation.

Other names
ThrombinActivated Factor IIActivated Factor XStuart-Prower factorF2aFXa
02

Mechanism of action

Direct or indirect inhibition of serine protease activity to prevent the conversion of prothrombin to thrombin (Xa inhibition) or fibrinogen to fibrin (IIa inhibition).

03

Biological functions

Blood coagulationHemostasisProteolysisFibrin formationPlatelet activationProthrombin activationCell signaling via proteinase-activated receptors (PARs)
04

Disease associations

ThrombosisVenous thromboembolism (VTE)Deep vein thrombosis (DVT)Pulmonary embolism (PE)Atrial fibrillation (AF)StrokeMyocardial infarctionCardiovascular diseaseDisseminated intravascular coagulation (DIC)
05

Safety considerations

Major and minor bleeding (hemorrhage)Gastrointestinal bleedingIntracranial hemorrhageHeparin-induced thrombocytopenia (HIT)Drug-drug interactions (e.g., with CYP3A4 or P-gp inhibitors/inducers)Renal impairment affecting drug clearance
06

Interacting drugs

Rivaroxaban

12 more in the full profile.

07

Biomarkers

Anti-Xa activityProthrombin time (PT)International Normalized Ratio (INR)Activated partial thromboplastin time (aPTT)Thrombin time (TT)Dilute thrombin time (dTT)Ecarin clotting time (ECT)Activated clotting time (ACT)

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