VEGFR-1 Inhibitors
16 drugsAbout VEGFR-1
VEGFR-1 (Vascular Endothelial Growth Factor Receptor 1) is a receptor tyrosine kinase that regulates angiogenesis by binding VEGF and modulating endothelial cell behavior. Its signaling plays a crucial role in blood vessel formation and vascular homeostasis.
Human genetic studies provide strong support for VEGFR-1 as a therapeutic target (max score 0.85), with variants linked to skeletal abnormalities (0.85), and coronary artery disease (0.84). These findings support therapeutic interventions modulating VEGFR-1 activity.
VEGFR-1 is targeted by 10 approved small molecule drugs including CABOMETYX, SORAFENIB TOSYLATE and INLYTA, spanning oncology (4 drugs) and other therapeutic areas (6 drugs). The first drug was approved in 2005 (NEXAVAR) and the most recent in 2023 (FRUZAQLA).
VEGFR-1 Genetic Evidence Strong
VEGFR-1 has strong genetic support with a max score of 0.85 linked to skeletal abnormalities.
Strong genetic support suggests a higher likelihood of clinical success, potentially justifying increased investment in VEGFR-1 targeted 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 VEGFR-1 Drugs
Ten companies have approved VEGFR-1 targeting drugs, including Viatris, NOVUGEN and EXELIXIS.
A fragmented competitive landscape suggests relatively low barriers to entry for new VEGFR-1 inhibitors.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| RETEVMO | Eli Lilly | 2020 | 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 |
| PAZOPANIB HYDROCHLORIDE | EUGIA PHARMA | 2023 | 2 |
| FOTIVDA | AVEO PHARMS | 2021 | 1 |
| FRUZAQLA | Takeda | 2023 | 1 |
| COMETRIQ | EXELIXIS | 2012 | 1 |
| RESNIBEN | AZURITY | - | - |
VEGFR-1 Drug Modality Landscape
Modalities
Routes of Administration
VEGFR-1 is amenable to small molecule drugs, with oral options available for convenient dosing.
The absence of antibody or protein modalities represents a whitespace opportunity for novel VEGFR-1 targeting strategies.
VEGFR-1 Clinical Trials 1,788 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on VEGFR-1. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 550 | 349 | 93 | 106 | 79% |
| Phase 2 | 987 | 439 | 202 | 339 | 68% |
| Phase 3 | 212 | 102 | 28 | 82 | 78% |
| 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-1 drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting VEGFR-1. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
VEGFR-1 Drug Approval Timeline (2005 - 2023)
The approval timeline spans 19 years, from 2005 to 2023.
Continued approvals indicate sustained interest, but recent approvals may signal increasing market saturation.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 14 companies competing
- • Market share by company
Full Drug Portfolio
- • All 16 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 16-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 577 (139 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-1. A trial counts if an approved drug acting on VEGFR-1 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.