Factor Xa Inhibitors
21 drugsAbout Factor Xa
Factor Xa (F10) is a serine protease essential for blood coagulation, catalyzing prothrombin to thrombin conversion within the prothrombinase complex. This pivotal step in the coagulation cascade makes it a key regulator of clot formation and a target for antithrombotic therapies.
Human genetics strongly support Factor Xa as a drug target, with a maximum genetic score of 0.96 linking F10 to 17 diseases. Loss-of-function variants are associated with increased risk of factor X deficiency (score 0.96), suggesting activation may be beneficial.
Factor Xa is targeted by 19 FDA-approved small molecule drugs, including XARELTO and ELIQUIS SPRINKLE. These drugs, developed by companies like Pfizer and Bristol-Myers Squibb, are primarily used in cardiovascular applications.
Factor Xa Genetic Evidence Strong
Genetic evidence strongly supports Factor Xa's role in multiple diseases, with a maximum score of 0.96.
Strong genetic support suggests that targeting Factor Xa has a higher likelihood of clinical success.
💡 Why activation?
- • Loss-of-function variants increase disease risk (OR > 1) — restoring function may help
- • 67% directional consistency across 3 traits
- • Strong signal in hematologic disease, cardiovascular disease pathways
Cross-Disease Effects
Trade-off: ModerateDirection of Effect
67% alignedEvidence Across Diseases
17 totalGWAS and other genetic studies link F10 to 17 diseases.
Loss-of-function causes disease; activation may help
Inhibiting this target may be therapeutic
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for F10 colocalize with these GWAS traits, providing causal evidence that gene expression changes drive disease risk.
Understanding these scores
Association Score (0-1): Combines all evidence types (genetic, literature, drugs, animal models). Higher = more evidence linking target to disease. This is a ranking heuristic, not a confidence score.
L2G Score: Open Targets uses a machine learning model (Locus-to-Gene) to predict which gene is causal at each GWAS locus. L2G=0.5 means ~50% probability of being the causal gene. Only associations with L2G > 0.05 are included.
Odds Ratio (OR): From gene burden studies (UK Biobank, AstraZeneca PheWAS). Measures how loss-of-function variants affect disease risk. OR<1 = protective (inhibiting target may help), OR>1 = risk (losing function causes disease).
Beta (β): Effect size for continuous traits. β<0 = protective, β>0 = risk.
Clinical Translation (~1.8x): Based on Nelson et al. 2015: drug targets with genetic evidence have ~2x higher success rates in clinical trials. We estimate: Strong support (score ≥0.7) → ~1.8x, Moderate (0.3-0.7) → ~1.3x, Weak → baseline.
Colocalization (H4): Tests whether a GWAS signal and an eQTL/pQTL signal share the same causal variant. H4 is the posterior probability that both traits are associated AND share a causal variant. H4 > 0.8 = strong evidence that gene expression/protein levels drive disease risk. This links genetic variation → gene expression → disease, supporting the target-disease connection.
Top Factor Xa Drugs
Ten companies have approved Factor Xa drugs, with Pfizer and Bristol-Myers Squibb as key players.
The presence of established companies suggests high barriers to entry for new competitors.
Factor Xa Drug Modality Landscape
Modalities
Routes of Administration
Factor Xa is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or peptides could provide a competitive advantage.
Factor Xa Clinical Trials 587 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on Factor Xa. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 100 | 88 | 7 | 5 | 93% |
| Phase 2 | 118 | 69 | 28 | 21 | 71% |
| Phase 3 | 179 | 102 | 32 | 45 | 76% |
| Phase 4 | 190 | 109 | 26 | 54 | 81% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Phase 3 Readout Calendar Pro
2 Phase 3 trials testing approved Factor Xa drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting Factor Xa. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
Factor Xa Drug Approval Timeline (1972 - 2025)
Venous Thrombosis
Venous Thrombosis
HEPARIN SODIUM IN SODIUM CHLORIDE INJECTION is indicated ...
Venous Thrombosis
Venous Thrombosis
Venous Thrombosis
The first Factor Xa drug was approved in 1972, with the most recent approval in 2025, spanning 54 years.
The continued approval of new Factor Xa drugs indicates sustained interest and potential for further innovation.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 12 companies competing
- • Market share by company
Full Drug Portfolio
- • All 21 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 21-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 350 (59 companies)
- • Completion rates by condition
Full summary • All drugs • Genetic evidence • Trials • Timeline
How We Count Trials
- Trials: phase 1-4 interventional trials on ClinicalTrials.gov that started in 2008 or later and test an FDA-approved drug acting on Factor Xa. A trial counts if an approved drug acting on Factor Xa is in any arm, including as a comparator, and a trial that tests two such drugs counts once. Trials that test only unapproved drugs are not counted. A trial listed as phase 1/2 counts as phase 1, and phase 2/3 as phase 2.
- Active: recruiting, not yet recruiting, enrolling by invitation, or active and no longer recruiting.
- Completion rate: of the trials that have ended, the share marked Completed rather than Terminated or Withdrawn. Completed means the trial ended as planned; it does not mean the drug worked. Suspended trials are not counted as ended.
- Stopped: terminated or withdrawn. Trials stop for many reasons, including slow enrolment and business decisions, not only safety or efficacy.
- Sponsors: the lead sponsor of each trial. Companies are the sponsors ClinicalTrials.gov classes as industry; the rest are universities, hospitals, cooperative groups, government bodies and individuals.