HER4 Inhibitors
4 drugsAbout HER4
Human Epidermal Growth Factor Receptor 4 (HER4) is a receptor tyrosine kinase in the EGFR/ErbB family, involved in cell signaling pathways. It plays a role in cell growth, differentiation, and survival, making it a relevant target for drug development.
Human genetic studies provide strong validation for HER4 as a therapeutic target, with variants linked to skeletal system abnormalities (score 0.89), polycystic ovary syndrome (score 0.88), and atrial fibrillation (score 0.84). Strong eQTL/pQTL signals further support HER4's role in disease.
HER4 is targeted by 4 FDA-approved small molecule drugs, including TAGRISSO, GILOTRIF, NERLYNX, and VIZIMPRO. These drugs are primarily used in oncology (3 drugs), with one drug targeting a different therapeutic area.
HER4 Genetic Evidence Strong
ERBB4 has strong genetic support with a max score of 0.89 linked to skeletal abnormalities.
Strong genetic support suggests that clinical trials targeting genetically validated indications may have a higher probability of success.
Evidence Across Diseases
20 totalGWAS and other genetic studies link ERBB4 to 37 diseases.
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for ERBB4 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 HER4 Drugs
Four companies have approved drugs targeting HER4: Boehringer Ingelheim, PUMA BIOTECH, Pfizer, and AstraZeneca.
The presence of four companies indicates a moderately competitive landscape, suggesting potential entry barriers for new players.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| GILOTRIF | Boehringer Ingelheim | 2013 | 1 |
HER4 Drug Modality Landscape
Modalities
Routes of Administration
HER4 is amenable to small molecule drugs, with oral options available for convenient dosing.
The exclusive use of small molecules suggests an opportunity to explore other modalities like antibodies or fusion proteins.
HER4 Clinical Trials 370 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on HER4. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 133 | 61 | 25 | 46 | 71% |
| Phase 2 | 187 | 70 | 24 | 92 | 74% |
| Phase 3 | 44 | 12 | 4 | 28 | 75% |
| Phase 4 | 6 | 4 | 1 | 1 | 80% |
Top Sponsors
By Modality
Top Conditions
Phase 3 Readout Calendar Pro
1 Phase 3 trial testing approved HER4 drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting HER4. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
HER4 Drug Approval Timeline (2013 - 2017)
The first HER4-targeting drug was approved in 2013 (GILOTRIF), with the most recent approval in 2018 (VIZIMPRO).
The approval timeline indicates a relatively recent interest in HER4, but a potential saturation as no new drugs have been approved since 2018.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 4 companies competing
- • Market share by company
Full Drug Portfolio
- • All 4 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 4-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 177 (51 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 HER4. A trial counts if an approved drug acting on HER4 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.