TYRO3 Inhibitors
3 drugsAbout TYRO3
TYRO3 is a receptor tyrosine kinase involved in cell communication, influencing cell growth, survival, and differentiation. Aberrant signaling through these pathways can contribute to a variety of diseases.
Human genetic studies provide moderate support for TYRO3 as a therapeutic target, with variants linked to metabolic syndrome (score 0.57) and moderate albuminuria (score 0.53). Colocalization analysis reveals 20 strong eQTL/pQTL signals (max H4: 1.00).
TYRO3 is targeted by 3 FDA-approved small molecule drugs: CABOMETYX, COMETRIQ, and RESNIBEN. These drugs are developed by EXELIXIS, AZURITY, and EXELIXIS INC for other therapeutic areas.
TYRO3 Genetic Evidence Moderate
Genetic evidence offers moderate support for TYRO3, with a max score of 0.57.
Further investigation of high H4 colocalization signals may reveal novel causal relationships.
Evidence Across Diseases
13 totalGWAS and other genetic studies link TYRO3 to 13 diseases.
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for TYRO3 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 TYRO3 Drugs
EXELIXIS, AZURITY, and EXELIXIS INC are the companies with approved TYRO3-targeting drugs.
The presence of multiple players suggests a competitive market, requiring a strong value proposition for new entrants.
TYRO3 Drug Modality Landscape
Modalities
Routes of Administration
TYRO3 is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or PROTACs could provide differentiation.
TYRO3 Clinical Trials 233 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on TYRO3. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 62 | 26 | 10 | 26 | 72% |
| Phase 2 | 138 | 54 | 21 | 61 | 72% |
| Phase 3 | 28 | 5 | 4 | 19 | 56% |
| Phase 4 | 5 | 1 | 0 | 4 | 100% |
Top Sponsors
By Modality
Top Conditions
Phase 3 Readout Calendar Pro
3 Phase 3 trials testing approved TYRO3 drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting TYRO3. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
TYRO3 Drug Approval Timeline (2012 - 2016)
The first drug was approved in 2012 (COMETRIQ), and the most recent in 2016 (CABOMETYX).
The relatively short approval span suggests a potentially unsaturated market with room for innovation.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 2 companies competing
- • Market share by company
Full Drug Portfolio
- • All 3 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 3-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 106 (18 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 TYRO3. A trial counts if an approved drug acting on TYRO3 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.