VEGFR-2 Inhibitors
18 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.
VEGFR-2 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 VEGFR-2 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 | Company | Approved | Indications |
|---|---|---|---|
| SUTENT | CPPI CV | 2006 | 4 |
| STIVARGA | Bayer | 2012 | 3 |
| SUNITINIB MALATE | Dr. Reddy's | 2021 | 3 |
| INLYTA | PF PRISM CV | 2012 | 3 |
| SORAFENIB TOSYLATE | YABAO PHARM | 2020 | 3 |
| OFEV | Boehringer Ingelheim | 2014 | 3 |
| NEXAVAR | Bayer | 2005 | 3 |
| VOTRIENT | Novartis | 2009 | 2 |
| GAVRETO | RIGEL PHARMS | 2020 | 2 |
| PAZOPANIB HYDROCHLORIDE | EUGIA PHARMA | 2023 | 2 |
| FOTIVDA | AVEO PHARMS | 2021 | 1 |
| QINLOCK | DECIPHERA PHARMS | 2020 | 1 |
| FRUZAQLA | Takeda | 2023 | 1 |
| COMETRIQ | EXELIXIS | 2012 | 1 |
| RESNIBEN | AZURITY | - | - |
VEGFR-2 Drug Modality Landscape
Modalities
Routes of Administration
VEGFR-2 is druggable by both biologics (1) and small molecules (17), indicating broad therapeutic accessibility.
The exclusive use of small molecules indicates a whitespace opportunity for alternative modalities like antibodies or fusion proteins.
📈 Modality Evolution
Small molecules pioneered VEGFR-2 targeting (2005), with antibodies entering more recently (2014).
VEGFR-2 Clinical Trials 1,921 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on VEGFR-2. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 585 | 363 | 103 | 117 | 78% |
| Phase 2 | 1067 | 481 | 213 | 366 | 69% |
| Phase 3 | 230 | 113 | 30 | 87 | 79% |
| Phase 4 | 39 | 24 | 4 | 11 | 86% |
Top Sponsors
By Modality
Top Conditions
Phase 3 Readout Calendar Pro
8 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.
VEGFR-2 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
- • 16 companies competing
- • Market share by company
Full Drug Portfolio
- • All 18 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 18-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 602 (154 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 VEGFR-2. A trial counts if an approved drug acting on VEGFR-2 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.