FLT3 Inhibitors
17 drugsAbout FLT3
FMS-Like Tyrosine Kinase 3 (FLT3) is a receptor tyrosine kinase involved in hematopoietic cell development. It regulates cell survival, proliferation, and differentiation, making it a key target in oncology.
FLT3 is genetically linked to 16 diseases, including skeletal abnormalities (score 0.85) and hypothyroidism (score 0.77), providing strong support for therapeutic intervention. Loss-of-function variants are protective against rheumatoid arthritis, suggesting inhibition is a viable strategy.
FLT3 is targeted by 10 FDA-approved small molecule drugs, including SUTENT, RYDAPT, and INREBIC. These drugs are used in oncology (4 drugs) and other therapeutic areas (6 drugs), with approvals spanning from 2006 to 2023.
FLT3 Genetic Evidence Strong
FLT3 has strong genetic support with a maximum score of 0.85 linked to skeletal abnormalities.
The strong genetic support suggests a higher probability of clinical success for FLT3-targeting therapies.
💡 Why inhibition?
- • Loss-of-function variants reduce disease risk (OR < 1)
- • 100% directional consistency across 1 traits
- • Strong signal in immune system disease, musculoskeletal or connective tissue disease, phenotype pathways
Cross-Disease Effects
Trade-off: LowDirection of Effect
100% alignedEvidence Across Diseases
16 totalGWAS and other genetic studies link FLT3 to 16 diseases.
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for FLT3 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 FLT3 Drugs
Nine companies have approved FLT3-targeting drugs, including NATCO PHARMA and Bristol-Myers Squibb.
The fragmented competitive landscape suggests relatively low barriers to entry for new FLT3-targeting therapies.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| INREBIC | Bristol-Myers Squibb | 2019 | 3 |
| SUNITINIB MALATE | Dr. Reddy's | 2021 | 3 |
| SORAFENIB TOSYLATE | YABAO PHARM | 2020 | 3 |
| OFEV | Boehringer Ingelheim | 2014 | 3 |
| NEXAVAR | Bayer | 2005 | 3 |
| GAVRETO | RIGEL PHARMS | 2020 | 2 |
| ICLUSIG | Takeda | 2012 | 2 |
| TURALIO | DAIICHI SANKYO INC | 2019 | 1 |
| ALUNBRIG | Takeda | 2017 | 1 |
| VANFLYTA | DAIICHI SANKYO INC | 2023 | 1 |
| COMETRIQ | EXELIXIS | 2012 | 1 |
| VONJO | SOBI | 2022 | 1 |
| XOSPATA | ASTELLAS | 2018 | 1 |
| RESNIBEN | AZURITY | - | - |
FLT3 Drug Modality Landscape
Modalities
Routes of Administration
FLT3 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.
FLT3 Clinical Trials 1,127 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on FLT3. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 407 | 245 | 78 | 83 | 76% |
| Phase 2 | 538 | 263 | 138 | 134 | 66% |
| Phase 3 | 153 | 78 | 24 | 51 | 76% |
| Phase 4 | 29 | 19 | 3 | 7 | 86% |
Top Sponsors
By Modality
Top Conditions
Phase 3 Readout Calendar Pro
4 Phase 3 trials testing approved FLT3 drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting FLT3. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
FLT3 Drug Approval Timeline (2005 - 2023)
The first FLT3-targeting drug was approved in 2006, with the most recent approval in 2023.
The continued approval of FLT3 inhibitors indicates sustained interest and potential for further development in this area.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 14 companies competing
- • Market share by company
Full Drug Portfolio
- • All 17 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 17-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 410 (106 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 FLT3. A trial counts if an approved drug acting on FLT3 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.