VEGFR3 Inhibitors
6 drugsAbout VEGFR3
VEGFR3 (Vascular Endothelial Growth Factor Receptor 3) is a tyrosine kinase receptor essential for lymphangiogenesis. It plays a crucial role in the formation of lymphatic vessels during development and in pathological conditions.
Human genetic studies provide strong validation for VEGFR3 as a therapeutic target, with variants linked to lymphatic malformation 1 (score 0.95), congenital heart defects (0.89), and Milroy disease (0.85). Loss-of-function variants are associated with increased disease risk, suggesting activation may be beneficial.
VEGFR3 is targeted by 6 FDA-approved drugs, all of which are small molecules, including LENVIMA, RETEVMO, and SUTENT. These drugs are used across oncology, respiratory diseases, and other therapeutic areas.
Strategic Insights
ℹ️ How we calculate- Validated target with strong trial activity and 81% attractiveness score.
Human Genetic Evidence Strong
Strong genetic evidence supports VEGFR3's role in lymphatic and cardiovascular development, with a max score of 0.95.
Strong genetic support increases clinical success probability; prioritize agonist therapies given LoF risk.
💡 Why activation?
- • Loss-of-function variants increase disease risk (OR > 1) — restoring function may help
- • 100% directional consistency across 3 traits
- • Strong signal in cardiovascular disease, genetic, familial or congenital disease, hematologic disease pathways
Cross-Disease Effects
Trade-off: LowDirection of Effect
100% alignedEvidence Across Diseases
11 totalGWAS and other genetic studies link FLT4 to 11 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 FLT4 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 Drugs
Six companies have approved VEGFR3-targeting drugs, including EISAI INC, Eli Lilly, and Bayer.
The presence of multiple established players suggests a moderately competitive market with potential entry barriers.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| STIVARGA | Bayer | 2012 | 3 |
| SUNITINIB MALATE | Dr. Reddy's | 2021 | 3 |
| OFEV | Boehringer Ingelheim | 2014 | 3 |
Drug Modality Landscape
Modalities
Routes of Administration
VEGFR3 is amenable to small molecule drugs, with oral options available for convenient dosing.
Explore alternative modalities like antibodies or fusion proteins to differentiate from existing therapies.
Clinical Trials 983 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 248 | 156 | 28 | 63 | 85% |
| Phase 2 | 529 | 197 | 96 | 230 | 67% |
| Phase 3 | 170 | 93 | 18 | 59 | 84% |
| Phase 4 | 36 | 22 | 4 | 10 | 85% |
Top Sponsors
By Modality
Top Conditions
Phase 3 Readout Calendar Pro
6 Phase 3 trials testing approved VEGFR3 drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting VEGFR3. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
Drug Approval Timeline (2006 - 2021)
The first VEGFR3-targeting drug was approved in 2006, with the most recent in 2021.
The approval timeline indicates a sustained interest in VEGFR3 as a drug target, but potential 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 VEGFR3.
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