Plasminogen Inhibitors
4 drugsAbout Plasminogen
Plasminogen (PLG) is a key protein in blood coagulation and fibrinolysis, converted to plasmin to dissolve clots. Modulation of this process is crucial in therapeutic areas like cardiovascular medicine and rare diseases.
Human genetic studies strongly validate PLG as a therapeutic target (max score 0.90). Loss-of-function variants are associated with hypoplasminogenemia (0.90), hereditary angioedema (0.87), and protection against coronary artery disease (0.81), suggesting activation may be beneficial.
Four FDA-approved drugs target PLG, including ACTIVASE, TRANEXAMIC ACID, LYSTEDA and TNKASE. These include small molecules and biologics, developed by Roche, EUGIA PHARMA, and AMRING PHARMS.
Plasminogen Genetic Evidence Strong
Strong genetic evidence supports PLG as a drug target, with a maximum score of 0.90.
The strong genetic support for PLG may increase the probability 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 genetic, familial or congenital disease, hematologic disease, integumentary system disease pathways
Cross-Disease Effects
Trade-off: ModerateDirection of Effect
67% alignedEvidence Across Diseases
20 totalGWAS and other genetic studies link PLG to 47 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 PLG 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 Plasminogen Drugs
Three companies have approved drugs targeting PLG: EUGIA PHARMA, Roche, and AMRING PHARMS.
The presence of three main players suggests a moderately competitive market with potential entry barriers.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| TRANEXAMIC ACID | AM REGENT | 2011 | 2 |
Plasminogen Drug Modality Landscape
Modalities
Routes of Administration
Plasminogen is druggable by both biologics (2) and small molecules (1), indicating broad therapeutic accessibility.
Given the even split, there may be opportunities to develop novel modalities targeting PLG.
📈 Modality Evolution
Enzymes pioneered Plasminogen targeting (1987), with small molecules entering more recently (2009).
Plasminogen Clinical Trials 501 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on Plasminogen. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 29 | 17 | 4 | 8 | 81% |
| Phase 2 | 108 | 64 | 20 | 23 | 76% |
| Phase 3 | 163 | 79 | 27 | 56 | 75% |
| Phase 4 | 201 | 120 | 31 | 50 | 79% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Phase 3 Readout Calendar Pro
1 Phase 3 trial testing approved Plasminogen drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting Plasminogen. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
Plasminogen Drug Approval Timeline (1987 - 2009)
The first drug was approved in 1987 (ACTIVASE), and the most recent in 2011 (TRANEXAMIC ACID).
The approval timeline suggests a mature market, but new indications could drive renewed interest.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 3 companies competing
- • Market share by company
Full Drug Portfolio
- • All 4 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 4-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 317 (20 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 Plasminogen. A trial counts if an approved drug acting on Plasminogen 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.