VEGFR-2 Inhibitors
10 drugsAbout VEGFR-2
Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2) is a protein kinase receptor essential for angiogenesis, the formation of new blood vessels. It plays a critical role in normal development and wound healing. However, it also promotes tumor growth and spread.
VEGFR-2 is a compelling therapeutic target due to its involvement in angiogenesis. Human genetic studies provide strong validation for VEGFR-2 as a drug target (max score 0.92), with loss-of-function variants linked to endometriosis and female infertility. Inhibition is likely beneficial.
Ten FDA-approved drugs target VEGFR-2, including CABOMETYX, SORAFENIB TOSYLATE, and INLYTA. All are small molecules. These drugs are used in oncology and other therapeutic areas.
Human Genetic Evidence Strong
Genetic evidence strongly supports VEGFR-2 as a drug target with a maximum score of 0.92.
Strong genetic support suggests a higher probability of clinical success for VEGFR-2 targeted therapies.
💡 Why inhibition?
- • Loss-of-function variants reduce disease risk (OR < 1)
- • 100% directional consistency across 1 traits
- • Strong signal in reproductive system or breast disease pathways
Cross-Disease Effects
Trade-off: LowDirection of Effect
100% alignedEvidence Across Diseases
16 totalGWAS and other genetic studies link KDR to 16 diseases.
Inhibiting this target may be therapeutic
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for KDR 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
Ten companies have approved drugs targeting VEGFR-2, including Viatris, NOVUGEN, and EXELIXIS.
The presence of ten companies suggests a moderately competitive landscape with potential entry barriers for new players.
Drug Modality Landscape
Modalities
Routes of Administration
VEGFR-2 is amenable to small molecule drugs, with oral options available for convenient dosing.
The exclusive use of small molecules indicates a whitespace opportunity for alternative modalities like antibodies or fusion proteins.
Clinical Trials 1,053 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 348 | 218 | 67 | 61 | 76% |
| Phase 2 | 560 | 263 | 113 | 182 | 70% |
| Phase 3 | 118 | 56 | 17 | 45 | 77% |
| Phase 4 | 27 | 16 | 2 | 9 | 89% |
Top Sponsors
By Modality
Top Conditions
Phase 3 Readout Calendar Pro
7 Phase 3 trials testing approved VEGFR-2 drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting VEGFR-2. 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 (2005 - 2023)
The first VEGFR-2 targeting drug was approved in 2005 (NEXAVAR), with the most recent approval in 2023 (FRUZAQLA).
The 19-year approval span indicates a mature market, but recent approvals suggest continued innovation potential.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 10 companies competing
- • Market share by company
Full Drug Portfolio
- • All 10 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 10-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 523 clinical trials targeting VEGFR-2.
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