Thrombin Inhibitors
6 drugsAbout Thrombin
Thrombin (F2), a serine protease in the coagulation cascade, converts fibrinogen to fibrin, forming blood clots and playing a key role in hemostasis and thrombosis.
Human genetics strongly support Thrombin as a target, with variants linked to congenital prothrombin deficiency (score 0.94) and deep vein thrombosis (score 0.91); loss-of-function is protective.
Six FDA-approved small molecule drugs target Thrombin, including Dabigatran etexilate mesylate, Argatroban, and Bivalirudin, primarily for cardiovascular indications.
Strategic Insights
ℹ️ How we calculate- White space opportunity in Relapsed Hodgkin Lymphoma with only 1 trials.
Thrombin Genetic Evidence Strong
Strong genetic evidence links Thrombin to 42 diseases, with a max score of 0.94 for congenital prothrombin deficiency.
The strong genetic support suggests that clinical trials targeting genetically validated indications have a higher probability of 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, genetic, familial or congenital disease pathways
Cross-Disease Effects
Trade-off: ModerateDirection of Effect
67% alignedEvidence Across Diseases
20 totalGWAS and other genetic studies link F2 to 42 diseases.
Loss-of-function causes disease; activation may help
Loss-of-function causes disease; activation may help
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for F2 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 Thrombin Drugs
Six companies have approved Thrombin-targeting drugs, with Hetero Labs Ltd III leading with Dabigatran etexilate mesylate.
The relatively low number of companies suggests moderate barriers to entry, but also potential for market disruption.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| ANGIOMAX RTU | MAIA PHARMS INC | 2019 | 2 |
| ANGIOMAX | Novartis | 2000 | 2 |
| PRADAXA | Boehringer Ingelheim | 2010 | 1 |
Thrombin Drug Modality Landscape
Modalities
Routes of Administration
Thrombin is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or peptides could offer a competitive advantage in targeting Thrombin.
Thrombin Clinical Trials 139 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 53 | 47 | 4 | 2 | 92% |
| Phase 2 | 19 | 9 | 6 | 4 | 60% |
| Phase 3 | 22 | 17 | 5 | 0 | 77% |
| Phase 4 | 45 | 27 | 12 | 6 | 69% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Thrombin Drug Approval Timeline (2000 - 2020)
The first Thrombin inhibitor was approved in 2000 (Argatroban), with the most recent approval in 2020 (Dabigatran etexilate mesylate).
The approval timeline indicates continued interest in Thrombin as a target, but also suggests a potentially saturated market.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 6 companies competing
- • Market share by company
Full Drug Portfolio
- • All 6 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 6-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Competition: High (15 sponsors)
- • White space: 10 underexplored indications
- • Success rates by condition
Full summary • All drugs • Genetic evidence • Trials • Timeline
How We Calculate These Metrics
Target Attractiveness Score
A 0-100 score based on trial activity, sponsor diversity, and completion rates. Calculated from 138 clinical trials targeting Thrombin.
Completion rate: Percentage of trials that reached their planned endpoint. Trials terminated early, withdrawn, or suspended are not counted—these often indicate safety issues, lack of efficacy, or strategic pivots.
- Highly Attractive (80+): High trial activity, many sponsors, strong completion rates
- Attractive (60-79): Good trial activity and validation
- Moderate (40-59): Moderate interest from sponsors
- Low (under 40): Limited trial activity or validation concerns
Strategic Insights
Auto-generated insights based on trial analytics including competition intensity, white space opportunities, modality shifts, and failure patterns. We analyze trial sponsors, phases, indications, and outcomes.
Risk Signals
- High Competition: Many sponsors competing for this target (may reduce market opportunity)
- High Failure Risk: Low trial completion rates suggest development challenges
- Low Validation: Limited trial activity or poor outcomes indicate uncertain viability
- White Space Available: Underexplored indications present opportunities