Target intelligence / Profile preview

Factor XIa (FXIa)

Target
FXIa
Molecular classification
Serine protease, Enzyme
01

Overview

Factor XIa (FXIa) is the active, serine protease form of Factor XI, a key enzyme in the intrinsic pathway of blood coagulation. FXIa exists as a homodimer and plays a central role in amplifying the coagulation cascade by catalyzing the activation of factor IX to factor IXa, which subsequently leads to activation of factor X and ultimately thrombin generation. Inhibitors targeting FXI/FXIa are being developed as novel anticoagulants aiming to prevent or treat thromboembolic diseases while minimizing bleeding complications. It's important to consider that the protein Z-dependent protease inhibitor (ZPI) physiologically inhibits FXI(a).

Other names
Coagulation factor XIaActivated Factor XIPlasma thromboplastin antecedent (PTA) - activated
02

Mechanism of action

Inhibition of FXIa activity, preventing the activation of Factor IX and subsequent thrombin generation

03

Biological functions

Blood coagulationActivation of Factor IXThrombin generationAmplification of coagulation cascade
04

Disease associations

ThrombosisHeart attackStrokePeripheral artery disease
05

Safety considerations

Potential bleeding risk (although potentially lower than traditional anticoagulants)Development of inhibitors with minimal impact on hemostasis
06

Interacting drugs

FXIa inhibitors (small molecules, antibodies, aptamers, polypeptides, antisense oligonucleotides)

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