5-HT1A receptor Inhibitors
8 drugsAbout 5-HT1A receptor
The 5-HT1A receptor is a G protein-coupled receptor that binds serotonin, regulating mood, anxiety, and cognition in the CNS. As a key serotonin receptor subtype, it presents a valuable target for treating various CNS disorders.
Human genetic studies offer moderate support for 5-HT1A as a therapeutic target, with variants linked to menstrual cycle-dependent periodic fever (score 0.62) and obesity (score 0.37). Activation of the receptor is likely beneficial based on genetic evidence.
5-HT1A is targeted by 8 FDA-approved small molecule drugs, including ARIPIPRAZOLE, VRAYLAR and OPIPZA, all indicated for CNS disorders. Seven companies have approved drugs targeting 5-HT1A, including UNICHEM, AbbVie and XIAMEN LP PHARM CO.
Strategic Insights
ℹ️ How we calculate- White space opportunity in Weight Gain with only 2 trials.
Human Genetic Evidence Moderate
Genetic evidence offers moderate support for the 5-HT1A receptor as a drug target.
Further investigation of the genetic links to fever and obesity may reveal novel therapeutic opportunities.
💡 Why activation?
- • Gain-of-function variants reduce disease risk — enhancing activity may help
- • 100% directional consistency across 1 traits
- • Strong signal in nutritional or metabolic disease, phenotype pathways
Cross-Disease Effects
Trade-off: LowDirection of Effect
100% alignedEvidence Across Diseases
20 totalGWAS and other genetic studies link HTR1A to 25 diseases.
Activating this target may be therapeutic
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 Drugs
Seven companies have approved drugs, with UNICHEM, AbbVie, and XIAMEN LP PHARM CO leading the market.
The presence of multiple players suggests a competitive market, requiring a differentiated approach for new entrants.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| VRAYLAR | AbbVie | 2015 | 2 |
| ABILIFY ASIMTUFII | OTSUKA | 2023 | 2 |
| TRINTELLIX | Takeda | 2013 | 1 |
| ARISTADA INITIO KIT | ALKERMES INC | 2018 | 1 |
| ARISTADA | ALKERMES INC | 2015 | 1 |
Drug Modality Landscape
Modalities
Routes of Administration
5-HT1A 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.
Clinical Trials 293 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 47 | 42 | 0 | 5 | 100% |
| Phase 2 | 47 | 30 | 9 | 8 | 77% |
| Phase 3 | 108 | 85 | 18 | 5 | 83% |
| Phase 4 | 91 | 60 | 22 | 9 | 73% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Drug Approval Timeline (2011 - 2024)
Major Depressive Disorder
The first drug was approved in 2013, with the most recent approval in 2024, spanning 12 years.
The recent approval suggests continued interest and potential for further drug development in this area.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 7 companies competing
- • Market share by company
Full Drug Portfolio
- • All 8 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 8-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 140 clinical trials targeting 5-HT1A 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