5-HT3 receptor Inhibitors
6 drugsAbout 5-HT3 receptor
The 5-HT3 receptor (serotonin receptor subtype 3) is a ligand-gated ion channel crucial for neuronal signaling in the nervous system. As a key player, it mediates fast synaptic transmission and modulates neurotransmitter release.
Human genetic studies provide moderate support for HTR3A as a therapeutic target, with variants linked to hypermobility syndrome (score 0.38). This suggests that modulating 5-HT3 receptor activity could impact disease risk.
The 5-HT3 receptor is targeted by 6 FDA-approved small molecule drugs, including ONDANSETRON HYDROCHLORIDE and LOTRONEX. These drugs span therapeutic areas such as CNS disorders and other conditions.
Strategic Insights
ℹ️ How we calculate- White space opportunity in HIV Infection with only 3 trials.
Human Genetic Evidence Moderate
Genetic evidence offers moderate support, with a max score of 0.38 linking HTR3A to hypermobility syndrome.
Further research into high scoring indications could reveal novel therapeutic opportunities.
Evidence Across Diseases
4 totalGWAS and other genetic studies link HTR3A to 4 diseases.
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
Six companies have approved drugs targeting the 5-HT3 receptor, including VIWIT PHARM and PF PRISM CV.
The relatively unconcentrated market suggests opportunities for new entrants with differentiated therapies.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| VARENICLINE TARTRATE | PHARMOBEDIENT | 2021 | 1 |
| TRINTELLIX | Takeda | 2013 | 1 |
| CHANTIX | PF PRISM CV | 2006 | 1 |
Drug Modality Landscape
Modalities
Routes of Administration
5-HT3 receptor is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or biologics could provide a competitive advantage.
Clinical Trials 436 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 73 | 60 | 9 | 4 | 87% |
| Phase 2 | 125 | 94 | 19 | 12 | 83% |
| Phase 3 | 98 | 77 | 11 | 10 | 88% |
| Phase 4 | 140 | 112 | 16 | 11 | 88% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Drug Approval Timeline (2000 - 2021)
The first drug was approved in 2000, with the most recent approval in 2021, spanning 22 years.
The continued approval of new drugs indicates sustained interest and potential for further innovation.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 6 companies competing
- • Market share by company
Full Drug Portfolio
- • All 6 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 6-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 213 clinical trials targeting 5-HT3 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