5-HT2 receptor Inhibitors
5 drugsAbout 5-HT2 receptor
The 5-HT2 receptor (5-hydroxytryptamine receptor) binds serotonin and modulates physiological processes in the central nervous system. As a prominent member of the serotonin receptor family, it is an important target for therapeutic intervention.
Human genetic studies provide moderate support for HTR2A 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.
Five FDA-approved small molecule drugs target 5-HT2 receptors, including FENFLURAMINE, FINTEPLA, ZYPREXA, and RALDESY. These drugs, developed by companies like Apotex, UCB INC, KAMAT and CHEPLAPHARM, span CNS and other therapeutic areas.
Strategic Insights
ℹ️ How we calculate- White space opportunity in Vomiting with only 2 trials.
5-HT2 receptor Genetic Evidence Moderate
Genetic evidence shows moderate support for HTR2A, with a max score of 0.55 for major depressive disorder.
Moderate genetic support suggests further validation studies are needed to increase confidence in clinical trials.
💡 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 5-HT2 receptor Drugs
Four companies have approved drugs, with Apotex, UCB INC, KAMAT and CHEPLAPHARM as top players.
The presence of multiple players suggests a moderately competitive market with potential for differentiation.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| ZYPREXA ZYDIS | CHEPLAPHARM | 2000 | 2 |
| RALDESY | KAMAT | 2024 | 1 |
5-HT2 receptor Drug Modality Landscape
Modalities
Routes of Administration
5-HT2 receptor is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or peptides could provide a competitive advantage.
5-HT2 receptor Clinical Trials 199 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 33 | 26 | 1 | 5 | 96% |
| Phase 2 | 44 | 23 | 9 | 10 | 72% |
| Phase 3 | 70 | 42 | 8 | 20 | 84% |
| Phase 4 | 52 | 33 | 10 | 9 | 77% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Phase 3 Readout Calendar Pro
5 Phase 3 trials testing approved 5-HT2 receptor drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting 5-HT2 receptor. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
5-HT2 receptor Drug Approval Timeline (1996 - 2024)
The first drug was approved in 1996 (ZYPREXA), and the most recent in 2024 (RALDESY), spanning 29 years.
The recent approval suggests continued interest, but a long span indicates potential saturation.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 4 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 133 clinical trials targeting 5-HT2 receptor.
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