EGFR Inhibitors
17 drugsAbout EGFR
EGFR (Epidermal Growth Factor Receptor) is a receptor tyrosine kinase on the cell surface crucial for cell growth, proliferation, and survival. Activated by growth factors, it triggers intracellular signaling cascades.
Human genetic studies provide strong validation for EGFR as a therapeutic target (max score 0.93), with variants linked to EGFR-related lung cancer (score 0.93) and head and neck squamous cell carcinoma (score 0.82). Loss-of-function variants are associated with increased risk of lung cancer, suggesting activation may be beneficial.
EGFR is targeted by 17 FDA-approved drugs, including TAGRISSO, RYBREVANT, and ERBITUX, primarily small molecules (11 drugs) and biologics. Applications span oncology (13 drugs) and other therapeutic areas (4 drugs).
EGFR Genetic Evidence Strong
EGFR has strong genetic support with a maximum score of 0.93 linking it to multiple diseases.
Strong genetic support suggests high confidence in target validity and increased likelihood of clinical success.
💡 Why activation?
- • Loss-of-function variants increase disease risk (OR > 1) — restoring function may help
- • 50% directional consistency across 2 traits
- • Strong signal in respiratory or thoracic disease, cancer or benign tumor pathways
Cross-Disease Effects
Trade-off: ModerateDirection of Effect
50% alignedEvidence Across Diseases
20 totalGWAS and other genetic studies link EGFR to 26 diseases.
Loss-of-function causes disease; activation may help
Gain-of-function causes disease; inhibition may help
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for EGFR 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 EGFR Drugs
Fourteen companies have approved drugs targeting EGFR, with Cipla, Takeda, and MSN among the top players.
The presence of many companies indicates a competitive landscape, requiring differentiated strategies for market entry.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| ERLOTINIB HYDROCHLORIDE | MSN | 2014 | 2 |
| NERLYNX | PUMA BIOTECH | 2017 | 1 |
| HYRNUO | Bayer | 2025 | 1 |
| RYBREVANT FASPRO | Johnson & Johnson | 2025 | 1 |
| ALUNBRIG | Takeda | 2017 | 1 |
| VIZIMPRO | Pfizer | 2018 | 1 |
| GEFITINIB | NATCO | 2022 | 1 |
| TYKERB | Novartis | 2007 | 1 |
| VECTIBIX | Amgen | 2006 | 1 |
| GILOTRIF | Boehringer Ingelheim | 2013 | 1 |
| CAPRELSA | Sanofi | 2011 | 1 |
| PORTRAZZA | Eli Lilly | 2015 | 1 |
| LAZCLUZE | Johnson & Johnson | 2024 | 1 |
| IRESSA | AstraZeneca | 2003 | - |
EGFR Drug Modality Landscape
Modalities
Routes of Administration
EGFR is druggable by both biologics (5) and small molecules (10), indicating broad therapeutic accessibility.
The dominance of small molecules suggests potential whitespace for novel biologic modalities targeting EGFR.
📈 Modality Evolution
Antibodies pioneered EGFR targeting (2004), with other biologics entering more recently (2021).
EGFR Clinical Trials 1,704 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on EGFR. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 611 | 306 | 132 | 169 | 70% |
| Phase 2 | 874 | 432 | 193 | 245 | 69% |
| Phase 3 | 198 | 89 | 26 | 83 | 77% |
| Phase 4 | 21 | 12 | 4 | 4 | 75% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Phase 3 Readout Calendar Pro
8 Phase 3 trials testing approved EGFR drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting EGFR. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
EGFR Drug Approval Timeline (2004 - 2025)
The first EGFR-targeting drug was approved in 2004, with the most recent approval in 2026, spanning 23 years.
The continued approval of EGFR-targeting drugs suggests sustained interest and potential for further innovation.
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: 553 (167 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 EGFR. A trial counts if an approved drug acting on EGFR 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.