5HT2A Inhibitors
5 drugsAbout 5HT2A
The 5HT2A receptor is a serotonin receptor in the central nervous system modulating neurological processes. As a key neurotransmitter receptor, it influences various brain functions, making it a target for therapeutic intervention.
Human genetic studies provide moderate support for 5HT2A as a therapeutic target, with variants linked to major depressive disorder (score 0.55) and color vision disorder (score 0.47). Loss-of-function variants are protective, suggesting inhibition may be beneficial.
5HT2A is targeted by 5 FDA-approved small molecule drugs, including SEROQUEL XR, INVEGA SUSTENNA and ERZOFRI, for CNS disorders. These drugs highlight the importance of 5HT2A in addressing CNS disorders.
Strategic Insights
ℹ️ How we calculate- White space opportunity in Bipolar I Disorder with only 1 trials.
5HT2A Genetic Evidence Moderate
Genetic evidence offers moderate support for 5HT2A, with a maximum score of 0.55 for major depressive disorder.
Moderate genetic support suggests further investigation into patient stratification strategies may improve clinical trial outcomes.
💡 Why inhibition?
- • Loss-of-function variants reduce disease risk (OR < 1)
- • 100% directional consistency across 1 traits
- • Strong signal in psychiatric disorder, nervous system disease pathways
Cross-Disease Effects
Trade-off: LowDirection of Effect
100% alignedEvidence Across Diseases
16 totalGWAS and other genetic studies link HTR2A to 16 diseases.
Inhibiting this target may be therapeutic
🔗 Colocalization Evidence 1 strong
max H4: 0.98eQTL/pQTL signals for HTR2A 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 5HT2A Drugs
Four companies have approved drugs targeting 5HT2A, including CHEPLAPHARM and Johnson & Johnson.
A relatively unconcentrated market suggests moderate barriers to entry for new competitors.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| ERZOFRI | LUYE INNOMIND PHARMA | 2024 | 2 |
| INVEGA TRINZA | Johnson & Johnson | 2015 | 1 |
5HT2A Drug Modality Landscape
Modalities
Routes of Administration
5HT2A is amenable to small molecule drugs, with oral options available for convenient dosing.
The absence of other modalities like antibodies or biologics represents a whitespace opportunity for innovation.
5HT2A Clinical Trials 139 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 23 | 21 | 1 | 1 | 95% |
| Phase 2 | 18 | 10 | 7 | 1 | 59% |
| Phase 3 | 36 | 27 | 6 | 3 | 82% |
| Phase 4 | 62 | 43 | 14 | 5 | 75% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
5HT2A Drug Approval Timeline (1997 - 2024)
The first 5HT2A-targeting drug was approved in 1997, with the most recent approval in 2024.
The 28-year span indicates a mature market, but recent approval suggests continued innovation potential.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 3 companies competing
- • Market share by company
Full Drug Portfolio
- • All 5 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 5-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Competition: High (15 sponsors)
- • White space: 10 underexplored indications
- • Success rates by condition
Full summary • All drugs • Genetic evidence • Trials • Timeline
How We Calculate These Metrics
Target Attractiveness Score
A 0-100 score based on trial activity, sponsor diversity, and completion rates. Calculated from 52 clinical trials targeting 5HT2A.
Completion rate: Percentage of trials that reached their planned endpoint. Trials terminated early, withdrawn, or suspended are not counted—these often indicate safety issues, lack of efficacy, or strategic pivots.
- Highly Attractive (80+): High trial activity, many sponsors, strong completion rates
- Attractive (60-79): Good trial activity and validation
- Moderate (40-59): Moderate interest from sponsors
- Low (under 40): Limited trial activity or validation concerns
Strategic Insights
Auto-generated insights based on trial analytics including competition intensity, white space opportunities, modality shifts, and failure patterns. We analyze trial sponsors, phases, indications, and outcomes.
Risk Signals
- High Competition: Many sponsors competing for this target (may reduce market opportunity)
- High Failure Risk: Low trial completion rates suggest development challenges
- Low Validation: Limited trial activity or poor outcomes indicate uncertain viability
- White Space Available: Underexplored indications present opportunities