GP IIb/IIIa Inhibitors
3 drugsAbout GP IIb/IIIa
Glycoprotein IIb/IIIa (GP IIb/IIIa), also known as integrin αIIbβ3, is a receptor on platelets crucial for aggregation and thrombus formation by binding fibrinogen and other ligands. Inhibition of this receptor blocks platelet aggregation, making it a significant drug target in cardiovascular therapeutics.
GP IIb/IIIa is strongly genetically validated (max score 0.97), with loss-of-function variants in ITGB3 linked to Glanzmann thrombasthenia and other bleeding disorders. Activation of GP IIb/IIIa is likely beneficial based on genetic evidence, suggesting potential for novel therapies.
GP IIb/IIIa is targeted by 3 FDA-approved drugs, including Eptifibatide (Integrilin) and Tirofiban hydrochloride (Aggastat), with small molecules (2 drugs) and peptides (1 drug) as modalities. These drugs are all indicated for cardiovascular conditions.
GP IIb/IIIa Genetic Evidence Strong
GP IIb/IIIa has strong genetic support with a max score of 0.97 linked to Glanzmann thrombasthenia.
Strong genetic support increases the likelihood of clinical success, warranting further investment in GP IIb/IIIa-targeted therapies.
💡 Why activation?
- • Loss-of-function variants increase disease risk (OR > 1) — restoring function may help
- • 100% directional consistency across 3 traits
- • Strong signal in hematologic disease, genetic, familial or congenital disease pathways
Cross-Disease Effects
Trade-off: LowDirection of Effect
100% alignedEvidence Across Diseases
20 totalGWAS and other genetic studies link ITGB3 to 22 diseases.
Loss-of-function causes disease; activation may help
Loss-of-function causes disease; activation may help
🔗 Colocalization Evidence 13 strong
max H4: 0.99eQTL/pQTL signals for ITGB3 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 GP IIb/IIIa Drugs
Three companies, including Slate Run Pharma and Medicure, have approved drugs targeting GP IIb/IIIa.
The limited number of companies suggests relatively low barriers to entry, but also a concentrated market.
GP IIb/IIIa Drug Modality Landscape
Modalities
Routes of Administration
GP IIb/IIIa is primarily targeted by small molecule modalities (67% of approved drugs).
Exploring alternative modalities beyond small molecules and peptides could offer a competitive advantage in the GP IIb/IIIa space.
📈 Modality Evolution
Small molecules pioneered GP IIb/IIIa targeting (1998), with peptides entering more recently (2015).
GP IIb/IIIa Clinical Trials 36 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on GP IIb/IIIa. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 5 | 2 | 2 | 1 | 50% |
| Phase 2 | 11 | 9 | 1 | 1 | 90% |
| Phase 3 | 10 | 4 | 0 | 6 | 100% |
| Phase 4 | 10 | 7 | 0 | 3 | 100% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
GP IIb/IIIa Drug Approval Timeline (1998 - 2021)
The first GP IIb/IIIa-targeting drug was approved in 1998, with the most recent approval in 2021.
The approval timeline indicates continued interest in GP IIb/IIIa as a target, but also potential market saturation.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 3 companies competing
- • Market share by company
Full Drug Portfolio
- • All 3 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 3-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 29 (2 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 GP IIb/IIIa. A trial counts if an approved drug acting on GP IIb/IIIa 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.