5-HT1A receptor Inhibitors
12 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.
5-HT1A receptor 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 5-HT1A receptor 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 |
|---|---|---|---|
| ARIPIPRAZOLE | Teva | 2015 | 3 |
| ABILIFY MAINTENA KIT | OTSUKA | 2013 | 3 |
| ABILIFY ASIMTUFII | OTSUKA | 2023 | 2 |
| TRINTELLIX | Takeda | 2013 | 1 |
| VILAZODONE HYDROCHLORIDE | Teva | 2019 | 1 |
| EXXUA | FABRE KRAMER | 2023 | 1 |
| ARISTADA | ALKERMES | 2015 | 1 |
| VIIBRYD | AbbVie | 2011 | 1 |
| ARISTADA INITIO KIT | ALKERMES | 2018 | 1 |
5-HT1A receptor 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.
5-HT1A receptor Clinical Trials 294 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on 5-HT1A receptor. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 39 | 35 | 0 | 4 | 100% |
| Phase 2 | 47 | 31 | 6 | 9 | 84% |
| Phase 3 | 108 | 83 | 17 | 8 | 83% |
| Phase 4 | 100 | 66 | 23 | 11 | 74% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
5-HT1A receptor Drug Approval Timeline (2011 - 2024)
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
- • 8 companies competing
- • Market share by company
Full Drug Portfolio
- • All 12 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 12-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 117 (38 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 5-HT1A receptor. A trial counts if an approved drug acting on 5-HT1A receptor 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.