VEGFR1 Inhibitors
6 drugsAbout VEGFR1
Vascular Endothelial Growth Factor Receptor 1 (VEGFR1) is a tyrosine kinase receptor crucial for angiogenesis, embryonic development, hematopoiesis, and vascular permeability regulation.
Human genetic studies provide strong validation for VEGFR1 as a therapeutic target (max score 0.85), with variants linked to skeletal abnormalities (0.85), coronary artery disease (0.84) and myocardial infarction (0.67). Colocalization analysis reveals 20 strong eQTL/pQTL signals (max H4: 1.00).
VEGFR1 is targeted by 6 FDA-approved small molecule drugs, including LENVIMA, RETEVMO, and SUTENT, primarily in oncology and other therapeutic areas.
Strategic Insights
ℹ️ How we calculate- Validated target with strong trial activity and 81% attractiveness score.
VEGFR1 Genetic Evidence Strong
Strong genetic evidence supports VEGFR1's role in various diseases, including skeletal abnormalities and cardiovascular conditions.
The strong genetic support suggests a higher likelihood of clinical success for VEGFR1-targeting therapies.
Evidence Across Diseases
19 totalGWAS and other genetic studies link FLT1 to 19 diseases.
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for FLT1 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 VEGFR1 Drugs
Six companies have approved VEGFR1-targeting drugs, including EISAI INC, NATCO PHARMA, and Eli Lilly.
The relatively fragmented market suggests moderate entry barriers for new VEGFR1-targeting therapies.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| OFEV | Boehringer Ingelheim | 2014 | 3 |
| SUNITINIB MALATE | MSN | 2021 | 3 |
| STIVARGA | Bayer | 2012 | 3 |
VEGFR1 Drug Modality Landscape
Modalities
Routes of Administration
VEGFR1 is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or fusion proteins could offer a competitive advantage.
VEGFR1 Clinical Trials 889 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 230 | 143 | 28 | 58 | 84% |
| Phase 2 | 509 | 182 | 95 | 227 | 66% |
| Phase 3 | 122 | 56 | 13 | 53 | 81% |
| Phase 4 | 28 | 17 | 3 | 8 | 85% |
Top Sponsors
By Modality
Top Conditions
Phase 3 Readout Calendar Pro
5 Phase 3 trials testing approved VEGFR1 drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting VEGFR1. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
VEGFR1 Drug Approval Timeline (2006 - 2021)
The first VEGFR1-targeting drug was approved in 2006, with the most recent approval in 2021.
The approval timeline indicates continued interest in VEGFR1 as a drug target, but potential market saturation.
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)
- • 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 722 clinical trials targeting VEGFR1.
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