Protein / target
Coagulation factor X
Protein at a glance
Biological role
Serine-type endopeptidase activity
Primary system
Cardiovascular system
Strongest disease association
factor X deficiency
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
9 approved · 7 in clinical development
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function
Factor Xa is a vitamin K-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor Va, calcium and phospholipid during blood clotting (PubMed:22409427, PubMed:39880037). Factor Xa activates pro-inflammatory signaling pathways in a protease-activated receptor (PAR)-dependent manner (PubMed:24041930, PubMed:30568593, PubMed:34831181, PubMed:18202198). Up-regulates expression of protease-activated receptors (PARs) F2R, F2RL1 and F2RL2 in dermal microvascular endothelial cells (PubMed:35738824). Triggers the production of pro-inflammatory cytokines, such as MCP-1/CCL2 and IL6, in cardiac fibroblasts and umbilical vein endothelial cells in PAR-1/F2R-dependent manner (PubMed:30568593, PubMed:34831181). Triggers the production of pro-inflammatory cytokines, such as MCP-1/CCL2, IL6, TNF/TNF, IL-1beta/IL1B, IL8/CXCL8 and IL18, in endothelial cells and atrial tissues (PubMed:24041930, PubMed:35738824, PubMed:9780208). Induces expression of adhesion molecules, such as ICAM1, VCAM1 and SELE, in endothelial cells and atrial tissues (PubMed:24041930, PubMed:35738824, PubMed:9780208). Increases expression of phosphorylated ERK1/2 in dermal microvascular endothelial cells and atrial tissues (PubMed:24041930, PubMed:35738824). Triggers activation of the transcription factor NF-kappa-B in dermal microvascular endothelial cells and atrial tissues (PubMed:24041930, PubMed:35738824). Activates pro-inflammatory and pro-fibrotic responses in dermal fibroblasts and enhances wound healing probably via PAR-2/F2RL1-dependent mechanism (PubMed:18202198). Activates barrier protective signaling responses in endothelial cells in PAR-2/F2RL1-dependent manner; the activity depends on the cleavage of PAR-2/F2RL1 by factor Xa (PubMed:22409427). Up-regulates expression of plasminogen activator inhibitor 1 (SERPINE1) in atrial tissues (PubMed:24041930)
Subcellular location
Domains and Gene Ontology detail (17)Hide
Domains & features
Gene Ontology
- Cendoplasmic reticulum lumen
- Cexternal side of plasma membrane
- Cextracellular region
- Cextracellular space
- CGolgi lumen
- Cplasma membrane
- Fcalcium ion binding
- Fphospholipid binding
- Fserine-type endopeptidase activity
- Pblood coagulation
- Ppositive regulation of cell migration
- Ppositive regulation of TOR signaling
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
View supporting evidenceHide supporting evidence
Proteolysis
- ·Factor Xa is a vitamin K-dependent glycoprotein that converts prothrombin to thrombin in…
- ·serine-type endopeptidase activity
- ·proteolysis
Immune signalling
- ·Factor Xa is a vitamin K-dependent glycoprotein that converts prothrombin to thrombin in…
Transcriptional regulation
- ·Factor Xa is a vitamin K-dependent glycoprotein that converts prothrombin to thrombin in…
Haemostasis
- ·blood coagulation
View underlying pathways (9)Hide underlying pathways
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Drugs targeting this protein
Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.
Coagulation factor X inhibitor
Appears in clinical studies involving ischemic stroke, atrial fibrillation, deep vein thrombosis, pulmonary embolism
Coagulation factor X inhibitor
Appears in clinical studies involving deep vein thrombosis, atrial fibrillation, pulmonary embolism, venous thromboembolism
ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.
Translational evidence
Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.
Strongest genetic associations
Human genetic evidence — the most direct causal link between this target and a disease.
Highest-confidence therapeutic associations
Diseases where a drug acting on this target has already reached clinical development.
Show all associationsHide all associations
Open Targets ranks 628 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.
Known drugs · 16 total
thrombotic disease · deep vein thrombosis · pulmonary embolism
deep vein thrombosis · venous thromboembolism · atrial fibrillation
deep vein thrombosis · atrial fibrillation · pulmonary embolism
Recurrent thrombophlebitis · venous thromboembolism · atrial fibrillation
blood coagulation disease · Multiple Organ Failure · cardiac transplant
angina pectoris · angina unstable · thrombotic disease
deep vein thrombosis
Reduced antithrombin III activity · blood coagulation disease · Disseminated intravascular coagulation
ischemic stroke · atrial fibrillation · deep vein thrombosis
thrombotic disease · pulmonary embolism · deep vein thrombosis
Tractability
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.
Show remaining trials (24)Hide
ClinicalTrials.gov via the drug-target graph.
Forefront confidence
Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.
The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.
What's happening now
Recent activity around this target, drawn from one canonical event stream. Every item is reached through 2 drugs that target this protein, so each event is news about that drug rather than about the protein directly.
- Regulatory approval
Approval: RIVAROXABAN (ANDA220874)
- Regulatory approval
Approval: RIVAROXABAN (ANDA208334)
- Regulatory approval
Approval: Rivaroxaban Koanaa (EMA)
- Regulatory approval
Approval: RIVAROXABAN (ANDA208534)
- Regulatory approval
Approval: Rivaroxaban Viatris (previously Rivaroxaban Mylan) (EMA)
- New publication2021 European Heart Rhythm Association Practical Guide on the Use of Non-Vitamin K Antagonist Oral Anticoagulants in Patients with Atrial Fibrillation.
- Regulatory approval
Approval: Rivaroxaban Accord (EMA)
- Regulatory approval
Approval: Apixaban Accord (EMA)
- New publicationApixaban for the Treatment of Venous Thromboembolism Associated with Cancer.
- New publicationA Controlled Trial of Rivaroxaban after Transcatheter Aortic-Valve Replacement.
- Safety communication
Drug Safety Update: Rivaroxaban (Xarelto▼): reminder that 15 mg and 20 mg tablets should be taken with food
- New publicationRivaroxaban with or without Aspirin in Stable Cardiovascular Disease.
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.