FYN Inhibitors
3 drugsAbout FYN
FYN is a non-receptor tyrosine kinase in the Src family, crucial for intracellular signaling pathways governing cell growth, differentiation, and survival. It plays a key role in transmitting signals from cell surface receptors to the nucleus, influencing gene expression and cellular behavior.
Human genetic studies provide strong support for FYN as a therapeutic target, with variants linked to hypothyroidism (score 0.77) and Parkinson's disease (score 0.74). Colocalization analysis reveals 20 strong eQTL/pQTL signals, further supporting its role in disease.
FYN is targeted by three FDA-approved small molecule drugs, including SPRYCEL, DASATINIB, and PHYRAGO, all for oncology indications. These drugs, developed by companies like Bristol-Myers Squibb and Apotex, highlight FYN's significance in cancer therapy.
FYN Genetic Evidence Strong
Genetic evidence strongly supports FYN's role in diseases like hypothyroidism and Parkinson's, with a max score of 0.77.
Strong genetic support suggests FYN modulation could be effective in treating genetically-linked diseases.
Evidence Across Diseases
15 totalGWAS and other genetic studies link FYN to 15 diseases.
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for FYN 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 FYN Drugs
The FYN drug market involves three companies: Apotex, HANDA THERAP, and Bristol-Myers Squibb.
Low market concentration suggests opportunities for new entrants with differentiated FYN inhibitors.
FYN Drug Modality Landscape
Modalities
Routes of Administration
FYN is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or PROTACs could provide a competitive advantage.
FYN Clinical Trials 218 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on FYN. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 89 | 45 | 31 | 13 | 59% |
| Phase 2 | 112 | 49 | 26 | 36 | 65% |
| Phase 3 | 11 | 6 | 1 | 4 | 86% |
| Phase 4 | 6 | 2 | 0 | 4 | 100% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
FYN Drug Approval Timeline (2006 - 2023)
The first FYN-targeting drug was approved in 2006 (SPRYCEL), with the most recent in 2023 (PHYRAGO).
Continued approvals indicate sustained interest, but increasing competition warrants careful market analysis.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 3 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: 111 (13 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 FYN. A trial counts if an approved drug acting on FYN 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.